Day: October 29, 2021

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Exploring the ability of dihydropyrimidine-5-carboxamide and 5-benzyl-2,4-diaminopyrimidine-based analogues for the selective inhibition of L. major dihydrofolate reductase published in 2021. Quality Control of 4-Methoxybenzaldehyde, Reprint Addresses Rashid, U (corresponding author), COMSATS Univ Islamabad, Dept Chem, Abbottabad Campus, Abbottabad 22060, Khyber Pakhtunk, Pakistan.. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde

To tackle leishmaniasis, search for efficient therapeutic drug targets should be pursued. Dihydrofolate reductase (DHFR) is considered as a key target for the treatment of leishmaniasis. In current study, we are interested in the design and synthesis of selective antifolates targeting DHFR from L. major. We focused on the development of new antifolates based on 3,4-dihydropyrimidine-2-one and 5-(3,5-dimethoxybenzyl)pyrimidine-2,4-diamine motif. Structure activity relationship (SAR) studies were performed on 4-phenyl ring of dihydropyrimidine (26-30) template. While for 5-(3,5-dimethoxybenzyl) pyrimidine-2,4-diamine, the impact of different amino acids (valine, tryptophan, phenylalanine, and glutamic acid) and two carbon linkers were explored (52-59). The synthesized compounds were assayed against LmDHFR. Compound 59 with the IC50 value of 0.10 mu M appeared as potent inhibitors of L. major. Selectivity for parasite DHFR over human DHFR was also determined. Derivatives 55-59 demonstrated excellent selectivity for LmDHFR. Highest selectivity for LmDHFR was shown by compounds 56 (SI = 84.5) and 58 (SI = 87.5). Compounds Antileishmanial activity against L. major and L. donovani promastigotes was also performed. To explore the interaction pattern of the synthesized compounds with biological macromolecules, the docking studies were carried out against homology modelled LmDHFR and hDHFR targets. (C) 2020 Elsevier Masson SAS. All rights reserved.

Quality Control of 4-Methoxybenzaldehyde. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Bibi, M; Qureshi, NA; Sadiq, A; Farooq, U; Hassan, A; Shaheen, N; Asghar, I; Umer, D; Ullah, A; Khan, FA; Salman, M; Bibi, A; Rashid, U or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In 2020.0 J AGR FOOD CHEM published article about ARYL-ALCOHOL OXIDASE; S-ADENOSYLMETHIONINE; VERATRYL ALCOHOL; DEGRADATION; FLAVORS; DEHYDROGENASE; BIOCONVERSION; PURIFICATION; ANISALDEHYDE; PRECURSORS in [Wickramasinghe, Purni C. K.; Munafo, John P., Jr.] Univ Tennessee, Dept Food Sci, Knoxville, TN 37996 USA in 2020.0, Cited 30.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. HPLC of Formula: C7H8O

Employing isotope incubation studies, the biosynthetic pathway leading to a series of benzylic derivatives was elucidated in the fermentation broth of the edible mushroom Ischnoderma resinosum (P. Karst). Twenty-six hydroxy- and methoxybenzylic derivatives were screened by gas chromatography-mass spectrometry (GC-MS) of which 13 were detected in the culture media. Results from the isotope incubation studies showed the transformation of both benzyl alcohol and benzoic acid into benzaldehyde. Benzaldehyde was then converted into 4-methoxybenzaldehyde via hydroxylation and subsequent methylation of the 4-C position. The resulting 4-methoxybenzaldehyde was then hydroxylated in the 3-C position followed by methylation into 3,4-dimethoxybenzaldehyde. Based on these findings, a novel metabolic scheme for the biosynthesis of benzylic derivatives in I. resinosum was proposed. The knowledge of the biosynthetic pathway was utilized to produce 4-hydroxy-3-methoxybenzaldehyde (vanillin) from 4-hydroxy-3-methoxybenzoic acid (vanillic acid). This is the first report to elucidate the biosynthetic pathway of benzyl derivatives and production of vanillin from I. resinosum.

About Benzyl Alcohol, If you have any questions, you can contact Wickramasinghe, PCK; Munafo, JP or concate me.. HPLC of Formula: C7H8O

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

I found the field of Chemistry very interesting. Saw the article Challenging synthesis of bisphosphonate derivatives with reduced steric hindrance published in 2021.0. Name: 4-Methoxybenzaldehyde, Reprint Addresses Scarso, A (corresponding author), Univ Ca Foscari Venezia, Dipartimento Sci Mol & Nanosistemi, Via Torino 155, I-30172 Venice, Ve, Italy.. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde

An alternative approach is reported for the synthesis of methyl ester protected bisphosphonate building blocks, such as methylene bisphosphonate, vinylidenebisphosphonate and aryl substituted prochiral vinylidenebisphosphonates, that cannot be obtained directly from dimethyl phosphite and dichloromethane. (C) 2021 Elsevier Ltd. All rights reserved.

Name: 4-Methoxybenzaldehyde. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Chiminazzo, A; Sperni, L; Fabris, F; Scarso, A or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Quality Control of 3-Hydroxybenzaldehyde. Recently I am researching about PROCESS WINDOWS; CHEMISTRY; REACTORS; LIQUID; SAFE, Saw an article supported by the Spanish MINECO [RTI2018-095588-B-I00]; European Regional Development Fund/European Social Fund, Investing in your future; FUSP-CEU [PC17/17]; Fundacion San Pablo-CEU. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Garcia-Lacuna, J; Dominguez, G; Blanco-Urgoiti, J; Perez-Castells, J. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde

A new synthesis of treprostinil is described using a plug flow reactor in two of the key steps. First, a Claisen rearrangement reaction is described in scaled flow at multigram amounts. Yields and selectivity of this step are sharply improved compared to those from previous syntheses. Second, the key Pauson-Khand reaction in flow is described under catalytic conditions with 5 mol% of cobalt carbonyl and only 3 equiv. of CO. Scaling up of this reaction safely ensures a good yield of an advanced intermediate which is transformed into treprostinil in three steps. Other improvements are the introduction of the carboxymethyl chain into the phenol from the beginning to reduce the protection-deprotection steps. The synthesis is completed in 14% global yield after 12 linear steps from (S)-epichlorhydrin.

Quality Control of 3-Hydroxybenzaldehyde. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Garcia-Lacuna, J; Dominguez, G; Blanco-Urgoiti, J; Perez-Castells, J or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about SUPERCRITICAL WATER GASIFICATION; PRESSURE AQUEOUS ENVIRONMENTS; HOT COMPRESSED WATER; HYDROGEN-PRODUCTION; BIOMASS GASIFICATION; CHEMICAL-REACTIONS; CELLULOSE; LIGNIN; CONVERSION; PYROLYSIS, Saw an article supported by the Scientific and Technological Research Council of Turkey (TUBITAK)Turkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [109M284]. Product Details of 150-19-6. Published in ELSEVIER in AMSTERDAM ,Authors: Gokkaya, DS; Cokkuvvetli, T; Saglam, M; Yuksel, M; Ballice, L. The CAS is 150-19-6. Through research, I have a further understanding and discovery of m-Methoxyphenol

In this study, poplar wood chips were gasified in sub-and supercritical water as biomass feedstock. Hydrothermal gasification experiments were performed to examine how the reaction temperature and different type of catalysts influence conversion efficiency. The effectiveness of commercially available [alkali catalyst; KOH], naturally available [mineral catalysts; Trona [Na-3(CO3)(HCO3)center dot 2H(2)O], Dolomite [CaMg(CO3)(2)] and Borax [Na2B4O7 center dot 10H(2)O] and laboratory-prepared catalysts [metal-impregnated activated carbons; (Ni/AC) and (Ru/AC)] have been demonstrated so as to shift the product distribution toward more desirable compounds. Gaseous compound yield was increased from 29.7% to 79.3% with respect to increasing temperature while liquid compound yield decreased from 27.6% to 1.1% and solid residue from 38.0% to 15.6%. The highest H-2 (20.1 mol/kg C in poplar) and CH4 (12.7 mol/kg C in poplar) yields were obtained with Ru/AC catalyst. Carboxylic acids and 5-methyl furfural were determined as the main liquid compounds. (C) 2019 Elsevier B.V. All rights reserved.

Product Details of 150-19-6. About m-Methoxyphenol, If you have any questions, you can contact Gokkaya, DS; Cokkuvvetli, T; Saglam, M; Yuksel, M; Ballice, L or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

HPLC of Formula: C9H7NO2. In 2021 ANTIVIR RES published article about NONCANONICAL POLY(A) POLYMERASE; POLYADENYLATION SIGNAL; MOLECULAR-BIOLOGY; STEM-LOOP; VIRUS; DEGRADATION; EXOSOME; TRAMP; DECAY; TRANSCRIPTS in [Block, Timothy M.; Zhou, Tianlun] Baruch S Blumberg Inst, Doylestown, PA 18902 USA; [Young, John A. T.] F Hoffmann La Roche Ltd, Roche Innovat Ctr Basel, Roche Pharma Res & Early Dev, Basel, Switzerland; [Javanbakht, Hassan] SQZ Biotechnol, 200 Arsenal Yards Blvd,Suite 210, Watertown, MA 02472 USA; [Sofia, Michael J.] Arbutus Biopharma Inc, 701 Vet Circle, Warminster, PA 18974 USA in 2021, Cited 69. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Inhibition of the host RNA polyadenylating polymerases, PAPD5 and PAPD7 (PAPD5/7), with dihydroquinolizinone, a small orally available, molecule, results in a rapid and selective degradation of hepatitis B virus (HBV) RNA, and hence reduction in the amounts of viral gene products. DHQ, is a first in class investigational agent and could represent an entirely new category of HBV antivirals. PAPD5 and PAPD7 are noncanonical, cell specified, polyadenylating polymerases, also called terminal nucleotidyl transferases 4B and 4A (TENT4B/A), respectively. They are involved in the degradation of poor-quality cell transcripts, mostly noncoding RNAs and in the maturation of a sub-set of transcripts. They also appear to play a role in shielding some mRNA from degradation. The results of studies with DHQ, along with other recent findings, provide evidence that repression of the PAPD5/7 arm of the cell RNA quality control pathway, causes a profound (multifold) reduction rather than increase, in the amount of HBV pre-genomic, pre-core and HBsAg mRNA levels in tissue culture and animal models, as well. In this review we will briefly discuss the need for new HBV therapeutics and provide background about HBV transcription. We also discuss cellular degradation of host transcripts, as it relates to a new family of anti-HBV drugs that interfere with these processes. Finally, since HBV mRNA maturation appears to be selectively sensitive to PAPD5/7 inhibition in hepatocytes, we discuss the possibility of targeting host RNA quality control as an antiviral strategy.

HPLC of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Block, TM; Young, JAT; Javanbakht, H; Sofia, MJ; Zhou, TL or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Category: indole-building-block. In 2021.0 J MOL LIQ published article about THERMOTROPIC LIQUID-CRYSTALS; MESOPHASE BEHAVIOR; SIDE-CHAIN; BENZOTHIAZOLE MESOGEN; AZOBENZENE; IMPACT; ORIENTATION; BENZOATES; MONOMERS; SERIES in [Kamal, Salwa J.; Mahmud, H. N. M. Ekramul; Abdullah, Iskandar] Univ Malaya, Fac Sci, Dept Chem, Kuala Lumpur 50603, Malaysia; [Salleh, Noordini M.; Velayutham, Thamil Selvi; Zahid, N. Idayu] Univ Malaya, Ctr Fundamental & Frontier Sci Nanostruct Self As, Fac Sci, Dept Chem, Kuala Lumpur 50603, Malaysia; [Gopal, Sanjeev R.; Velayutham, Thamil Selvi] Univ Malaya, Fac Sci, Low Dimens Mat Res Ctr, Dept Phys, Kuala Lumpur 50603, Malaysia; [Kamal, Salwa J.] Imam Abdulrahman Bin Faisal Univ, Coll Sci, Dept Chem, POB 1982, Dammam 31441, Saudi Arabia in 2021.0, Cited 46.0. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5.

The effect of introducing a lateral methyl substituent and the two different alkoxy terminal groups on the mesophase behavior of three-benzene-ring molecular core of azo-ester compounds bearing 2-methylbutoxy unit on the opposite terminal side (C1-C6) were explored. Their structures were confirmed by several spectroscopic techniques (Fourier transform infrared spectroscopy, H-1 and C-13 nuclear magnetic resonance spectroscopy). The mesomorphic properties of these compounds were studied by differential scanning calorimetry, polarized optical microscopy, and small- and wide-angle X-ray scattering. Except for the un-substituted terminals (C1 and C4), all other derivatives are liquid crystalline, exhibiting enantiotropic nematic liquid crystal phase. The alteration of the alkoxy chain length from methoxy to butoxy at the phenyl ester terminal group (ring A) for each set of laterally-neat and laterally methyl-substituted mesogens decreases the nematic temperature range. A decrease in the mesophase temperature range is also observed when a lateral methyl substituent is incorporated into phenylazo ring of the mesogenic core (ring C). Optical study demonstrated that their absorption spectra are identical in shape due to the structural similarities of the mesogenic core. The corresponding fluorescence spectra exhibited blue-emission with the laterally methyl substituted compounds having a relatively higher fluorescence intensity compared to that of its laterally un-substituted analogues. Furthermore, the laterally methyl-substituted derivatives were subjected to the planar alignment and their dielectric and electro-optic properties were investigated. The nematic phase of the aligned samples shows antiferroelectric switching behavior with spontaneous polarization, P-s similar to 5 mu C/cm(2). (C) 2021 Elsevier B.V. All rights reserved.

About Mequinol, If you have any questions, you can contact Kamal, SJ; Salleh, NM; Mahmud, HNME; Abdullah, I; Gopal, SR; Velayutham, TS; Zahid, NI or concate me.. Category: indole-building-block

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Authors Kratky, M; Svrckova, K; Vu, QA; Stepankova, S; Vinsova, J in MDPI published article about in [Kratky, Martin; Vu, Quynh Anh; Vinsova, Jarmila] Charles Univ Prague, Dept Organ & Bioorgan Chem, Fac Pharm Hradec Kralove, Akad Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic; [Svrckova, Katarina; Stepankova, Sarka] Univ Pardubice, Fac Chem Technol, Dept Biol & Biochem Sci, Studentska 573, Pardubice 53210, Czech Republic in 2021, Cited 31. Category: indole-building-block. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

Based on the broad spectrum of biological activity of hydrazide-hydrazones, trifluoromethyl compounds, and clinical usage of cholinesterase inhibitors, we investigated hydrazones obtained from 4-(trifluoromethyl)benzohydrazide and various benzaldehydes or aliphatic ketones as potential inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). They were evaluated using Ellman’s spectrophotometric method. The hydrazide-hydrazones produced a dual inhibition of both cholinesterase enzymes with IC50 values of 46.8-137.7 mu M and 19.1-881.1 mu M for AChE and BuChE, respectively. The majority of the compounds were stronger inhibitors of AChE; four of them (2-bromobenzaldehyde, 3-(trifluoromethyl)benzaldehyde, cyclohexanone, and camphor-based 2o, 2p, 3c, and 3d, respectively) produced a balanced inhibition of the enzymes and only 2-chloro/trifluoromethyl benzylidene derivatives 2d and 2q were found to be more potent inhibitors of BuChE. 4-(Trifluoromethyl)-N’-[4-(trifluoromethyl)benzylidene]benzohydrazide 2l produced the strongest inhibition of AChE via mixed-type inhibition determined experimentally. Structure-activity relationships were identified. The compounds fit physicochemical space for targeting central nervous systems with no apparent cytotoxicity for eukaryotic cell line together. The study provides new insights into this CF3-hydrazide-hydrazone scaffold.

Category: indole-building-block. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Kratky, M; Svrckova, K; Vu, QA; Stepankova, S; Vinsova, J or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

An article Synthesis and biological evaluation of Doxorubicin-containing conjugate targeting PSMA WOS:000463383800018 published article about RESISTANT PROSTATE-CANCER; MEMBRANE ANTIGEN PSMA; LU-177-PSMA-617 RADIOLIGAND THERAPY; GLUTAMATE CARBOXYPEPTIDASE II; MONOCLONAL-ANTIBODY; RADIATION-DOSIMETRY; INHIBITORS; PRODRUG; BIODISTRIBUTION; DESIGN in [Ivanenkov, Yan A.; Deyneka, Ekaterina, V; Trofimenko, Alexander, V; Aladinskaya, Anastasia, V; Puchinina, Maria M.] Moscow Inst Phys & Technol, 9 Inst Lane, Dolgoprudny City 141700, Moscow Region, Russia; [Ivanenkov, Yan A.; Machulkin, Alexey E.; Garanina, Anastasia S.; Skvortsov, Dmitry A.; Uspenskaya, Anastasia A.; Beloglazkina, Elena K.; Zyk, Nikolay, V; Koteliansky, Victor E.; Bezrukov, Dmitry S.; Riabykh, Grigory K.; Majouga, Alexander G.] Lomonosov Moscow State Univ, Chem Dept, Bldg 1-3,GSP 1, Moscow 119991, Russia; [Ivanenkov, Yan A.; Garanina, Anastasia S.; Majouga, Alexander G.] Natl Univ Sci & Technol MISiS, 9 Leninskiy Pr, Moscow 119049, Russia; [Ivanenkov, Yan A.] ChemDiv, San Diego, CA USA; [Ivanenkov, Yan A.] Russian Acad Sci, Inst Biochem & Genet, Ufa Sci Ctr, Oktyabrya Prospekt 71, Ufa 450054, Russia; [Bezrukov, Dmitry S.] Skolkovo Inst Sci & Technol, Skolkovo Innovat Ctr, Bldg 3, Moscow 143026, Russia; [Majouga, Alexander G.] Dmitry Mendeleev Univ Chem Technol Russia, Miusskaya Sq 9, Moscow 125047, Russia; [Vorobyeva, Nataliya S.] Centaura LLC, Moscow, Russia; [Sofronova, Alina A.] Lomonosov Moscow State Univ, Fac Bioengn & Bioinformat, Moscow, Russia; [Malyshev, Alexander S.] Lomonosov Moscow State Univ, Fac Med, Moscow, Russia in 2019.0, Cited 59.0. HPLC of Formula: C7H8O. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6

Prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II (GCPII), has recently emerged as a prominent biomarker of prostate cancer (PC) and as an attractive protein trap for drug targeting. At the present time, several drugs and molecular diagnostic tools conjugated with selective PSMA ligands are actively evaluated in different preclinical and clinical trials. In the current work, we discuss design, synthesis and a preliminary biological evaluation of PSMA-specific small-molecule carrier equipped by Doxorubicin (Dox). We have introduced an unstable azo-linker between Dox and the carrier hence the designed compound does release the active substance inside cancer cells thereby providing a relatively high Dox concentration in nuclei and a relevant cytotoxic effect. In contrast, we have also synthesized a similar conjugate with a stable amide linker and it did not release the drug at all. This compound was predominantly accumulated in cytoplasm and did not cause cell death. Preliminary in vivo evaluation has showed good efficiency for the degradable conjugate against PC3-PIP(PSMA(+))-containing xenograft mine. Thus, we have demonstrated that the conjugate can be used as a template to design novel analogues with improved targeting, anticancer activity and lower rate of potential side effects. 3D molecular docking study has also been performed to elucidate the underlying mechanism of binding and to further optimization of the linker area for improving the target affinity.

HPLC of Formula: C7H8O. About Benzyl Alcohol, If you have any questions, you can contact Ivanenkov, YA; Machulkin, AE; Garanina, AS; Skvortsov, DA; Uspenskaya, AA; Deyneka, EV; Trofimenko, AV; Beloglazkina, EK; Zyk, NV; Koteliansky, VE; Bezrukov, DS; Aladinskaya, AV; Vorobyeva, NS; Puchinina, MM; Riabykh, GK; Sofronova, AA; Malyshev, AS; Majouga, AG or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about DNA CLEAVAGE; ANTITUBERCULAR AGENTS; PYRIMIDINE HYBRIDS; SCAFFOLD, Saw an article supported by the UGC New Delhi, IndiaUniversity Grants Commission, India [F117.1/201617/RGNF-2015-17-SC-MAH-26074/(SAIII/Website)]; UGC-SWRO, Bangalore [F.2070-MRP/15-16/KAKA056/UGC-SWRO]. Published in ELSEVIER in AMSTERDAM ,Authors: Mane, SG; Reddy, DS; Katagi, KS; Kumar, A; Munnolli, RS; Kadam, NS; Akki, MC; Nagarajaiah, H; Joshi, SD. The CAS is 150-76-5. Through research, I have a further understanding and discovery of Mequinol. SDS of cas: 150-76-5

In this work, a series of new 8-[(substituted 2-oxo-2H-chromen-4-yOmethyl]-8-azaspiro[4.5]decane-7,9-dione derivatives (1a – 1l) is synthesized and characterized by H-1 NMR, C-13 NMR, FT-IR, GC-MS and elemental analysis. In addition, the structure of compound 1k has been elucidated using single crystal X-ray diffraction techniques. The synthesized compounds are screened for their anticancer and anti-TB activity. Preliminary anticancer results showed that compounds (1a- 1l) exhibit moderate to potent activity against MDA-MB-231, A549, HT-29 and Hela cancer cell lines. Compound if exhibited the most potent activity against MDA-MB-231cell line with IC50 value of 9.05 mu M concentration, compound lg and 1h showed potent activity against A549 cell line with IC50 value of 7.05 and 13.31 mu M concentration respectively. Compound 1j showed good cytotoxicity against Hela cell line with IC50 of 16.14 mu M, whereas, compound 1l is found to be moderately active against HT-29 cell line with IC50 of 18.07 mu M. Anti-tubercular activity revealed that compound 1c, 1d, 1g, 1h and 1j have significant activity against MTBH(37)Rv strain with MIC 0.78, 1.56, 0.19, 0.39 and 0.78 mu g/mL respectively. Further, to investigate the mechanism of anti-TB activity and detailed intermolecular interactions between the synthesized compounds, molecular docking studies are performed. (C) 2020 Elsevier B.V. All rights reserved.

About Mequinol, If you have any questions, you can contact Mane, SG; Reddy, DS; Katagi, KS; Kumar, A; Munnolli, RS; Kadam, NS; Akki, MC; Nagarajaiah, H; Joshi, SD or concate me.. SDS of cas: 150-76-5

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles