Tag: M.W=100-150

Category: indole-building-block. In 2019.0 RES CHEM INTERMEDIAT published article about MOLECULAR DOCKING; ORGANIC SELENIDES; TOPOISOMERASE-II; MICROTUBULE; ANTIOXIDANT; CELLS in [Bakherad, Zohreh; Fassihi, Afshin; Sadeghi-Aliabadi, Hojjat; Saghaie, Lotfollah] Isfahan Univ Med Sci, Sch Pharm & Pharmaceut Sci, Dept Med Chem, Esfahan 8174673461, Iran; [Safavi, Maliheh] Iranian Res Org Sci & Technol, Dept Biotechnol, Tehran 33535111, Iran; [Sepehri, Saghi] Ardabil Univ Med Sci, Sch Pharm, Dept Med Chem, Ardebil 5618953141, Iran; [Bakherad, Mohammad] Shahrood Univ Technol, Sch Chem, Shahrood, Iran; [Rastegar, Hossein] MOE & ME, Food & Drug Lab Res Ctr, Food & Drug Control Labs, Tehran, Iran; [Larijani, Bagher; Mahdavi, Mohammad] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Res Inst, Tehran, Iran in 2019.0, Cited 32.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

A series of novel imidazopyridine derivatives of indole has been synthesized. All the synthesized derivatives were evaluated for their antiproliferative activity against A-549, T-47D, Hep-G2 and MCF-7 human cancer cell lines. The results demonstrated that some of these derivatives exhibited moderate to excellent cytotoxic activities. Compounds 7a having a cyclohexyl ring substituted to the second amine of imidazopyridyl moiety and phenyl ring of the C-2 indole ring and 7f with a para-methylphenyl ring at the same position exhibited the highest activity against the A-594 cell line with IC50 of 11.48 mu M and 10.66 mu M, respectively. The results indicate that compounds 7a and 7f are more cytotoxic towards cancer cell lines compared with etoposide in vitro. In addition, compounds, 7d and 7j showed the most potent activity against Hep-G2, equal to etoposide as the standard drug. Also, most of the compounds were inactive against the T-47D and MCF-7 cell lines. The morphological analysis by the acridine orange/ethidium bromide double-staining test and flow cytometry analysis indicated that compounds 7a and 7f induced apoptosis in A-549 cells. Furthermore, in silico and in vitro results of the synthesized compounds showed good correlation with each other. Molecular docking results of the compounds of the 7a-k series with the cyclohexyl ring substituted to the second amine of the imidazopyridyl moiety compared with the 7l-t members with the t-butyl group at the same position confirmed the effect of the higher lipophilicity on hydrophobic interactions with the studied enzymes. Moreover, all the compounds showed higher affinity to tubulin than topoisomerase II alpha enzyme.

Category: indole-building-block. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Bakherad, Z; Safavi, M; Sepehri, S; Fassihi, A; Sadeghi-Aliabadi, H; Bakherad, M; Rastegar, H; Larijani, B; Saghaie, L; Mahdavi, M 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 HIGHLY ENANTIOSELECTIVE APPROACH; CYCLOADDITION; 4C+3C, Saw an article supported by the M.D. Anderson Foundation; University of Houston. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Li, J; Gilbertson, SR. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde. Category: indole-building-block

A diastereoselective [4 + 2] cycloisomerization of asymmetric allenyl dienes is reported. The asymmetric dienyl allenes are synthesized using the method reported by Ma. These substrates readily undergo diastereoselective intramolecular rhodium catalyzed [4 + 2] cycloisomerization analogous to thermal intramolecular Diels-Alder reactions. Overall, 29 examples are presented with tethers possessing nitrogen, oxygen, and carbon. Diastereoselectivities range from 99:1 to 90:10 in most examples.

Category: indole-building-block. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Li, J; Gilbertson, SR 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 Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation WOS:000483383900006 published article about INDOLE ALKALOIDS; ENDOPHYTIC FUNGUS; A-C; PENICILLIUM; BIOCHEMISTRY; PRODUCT; TUBULIN in [Kartsev, Victor] InterBioscreen, Moscow, Russia; [Geronikaki, Athina; Petrou, Anthi] Aristotle Univ Thessaloniki, Dept Pharm, Sch Hlth, Thessaloniki 54124, Greece; [Lichitsky, Boris] Zelinsky Inst Organ Chem, Moscow 119991, Russia; [Kostic, Marina; Smiljkovic, Marija; Sokovic, Marina] Univ Belgrade, Mycol Lab, Dept Plant Physiol, Inst Biol Res Sinisa Stankov, Bulevar Despota Stefana 142, Belgrade 11000, Serbia; [Sirakanyan, Samvel] Natl Acad Sci Republ Armenia, Sci Technol Ctr Organ & Pharmaceut Chem, Inst Fine Organ Chem AL Mnjoyan, Ave Azatutyan 26, Yerevan 0014, Armenia in 2019.0, Cited 48.0. Safety of 3-Hydroxybenzaldehyde. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4

Background: Griseofulvin – a mold metabolite produced by Penisilium griseofulvum is known as an antifungal drug. Objective: Thus, the goal of this paper is the design and synthesis of new griseofulvin derivatives and evaluation of their antifungal activity. Methods: Forty-two new compounds were synthesized using classical methods of organic synthesis and evaluated for their antimicrobial activity by microdilution method. Results: All forty-two new compounds exhibited very good activity against eight tested micromycetes with MIC ranging from 0.0075-0.055 mg/ml and MFC from 0.02-024 mg/ml. All compounds exhibited better activity than reference drugs ketoconazole (7-42 times) and bifonazole (3-16 fold). The most promising was compound 15. The most sensitive fungal was found to be T. viride, while the most resistant, as was expected, was A. fumigatus. It should be mentioned that most of compounds exhibited better activity than griseofulvin. The molecular docking studies revealed that the most active compound have the same hydrophobic and H-bonding interactions with Thr276 residue observed for griseofulvin forming 3 hydrogen bonds while griseofulvin only one. In general, the molecular docking results coincide with experimental. Conclusion: Forty-two giseofulvin derivatives were designed, synthesized and evaluated for antimicrobial activity. These derivatives revealed good antifungal activity, better than reference drugs ketoconazole, bifonazole, and griseofulvin as well.

About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Kartsev, V; Geronikaki, A; Petrou, A; Lichitsky, B; Kostic, M; Smiljkovic, M; Sokovic, M; Sirakanyan, S or concate me.. Safety of 3-Hydroxybenzaldehyde

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. Li, LX; Dong, L; Li, DD; Guo, Y; Liu, XH; Wang, YQ in [Li, Lingxiao; Dong, Lin; Li, Didi; Guo, Yong; Liu, Xiaohui; Wang, Yanqin] East China Univ Sci & Technol, Sch Chem & Mol Engn, Res Inst Ind Catalysis, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China published Hydrogen-Free Production of 4-Alkylphenols from Lignin via Self-Reforming-Driven Depolymerization and Hydrogenolysis in 2020.0, Cited 59.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

Lignin is constructed from methoxylated phenylpropanoid with plenty of hydroxys and methoxys. Its conversion to valuable products is extremely attractive but especially challenging without additional hydrogen sources. Herein we report a hydrogen-free production of 4-alkylphenols directly from native lignin via self-reforming-driven depolymerization and hydrogenolysis over Pt/NiAl2O4. This is the first example of acquiring 4-alkylphenols from native lignin. Using this strategy, high yields of 4-alkylphenols, 17.3 wt %, were obtained from birch lignin. Reaction pathway and mechanism studies revealed that this strategy initiates from the reforming of aliphatic hydroxys, followed by the cleavage of C-O linkages, and ends via demethoxylation over Pt/NiAl2O4. Moreover, the subsequent aqueous phase reforming of the as-formed methanol accelerates the whole process. This strategy realizes the one-pot production of 4-alkylphenols from lignin by fully utilizing the structural hydrogen in lignin and H2O, providing a low-cost and safe method of lignin valorization.

About 4′-Hydroxyacetophenone, If you have any questions, you can contact Li, LX; Dong, L; Li, DD; Guo, Y; Liu, XH; Wang, YQ 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 Mentese, E; Sokmen, BB in WILEY published article about MOLECULAR DOCKING; BIOLOGICAL-ACTIVITIES; BEARING TRIAZOLE; DERIVATIVES; ANTIOXIDANT; OXADIAZOLE in [Mentese, Emre] Recep Tayyip Erdogan Univ, Art & Sci Fac, Dept Chem, Rize, Turkey; [Sokmen, Bahar Bilgin] Giresun Univ, Fac Arts & Sci, Dept Chem, TR-28049 Giresun, Turkey in 2019.0, Cited 27.0. Quality Control of 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4

A novel series of N ‘-(substituted benzylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides and N ‘-(1-(substituted phenyl)ethylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides were synthesized and then studied for their urease inhibitory activities using thiourea as a standard drug. All newly synthesized compounds were found to exhibit potent inhibitory properties against urease enzyme in the range of IC50 = 0.0155 +/- 0.0039-0.0602 +/- 0.0071 mu M, when compared with the thiourea as standard (IC50 = 0.5115 +/- 0.0233 mu M). All target molecules were characterized by H-1-NMR, C-13-NMR, IR, and electrospray ionization mass spectrometry.

Quality Control of 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Mentese, E; Sokmen, BB 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

Field, T; Peterson, J; Ma, CC; Jagadesan, P; Da Silva, JP; Rubina, M; Ramamurthy, V; Givens, RS in [Field, Thomas; Peterson, Julie; Ma, Chicheng; Rubina, Marina; Givens, Richard S.] Univ Kansas, Dept Chem, Lawrence, KS 66045 USA; [Jagadesan, Pradeepkumar; Ramamurthy, V.] Univ Miami, Dept Chem, Coral Gables, FL 33124 USA; [Da Silva, Jose P.] Univ Algarve, CCMAR Ctr Marine Sci, Campus Gambelas, P-8005139 Faro, Portugal published Competing pathways for photoremovable protecting groups: the effects of solvent, oxygen and encapsulation in 2020.0, Cited 58.0. Name: 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

Extending the applications of Photoremovable Protecting Groups (PPGs) to cage phenols has generally met with unusually complex PPG byproducts. In this study, we demonstrate that thep-hydroxyphenacyl (pHP) cage for both simple and complex phenolics, including tyrosine, dispenses free phenols. With the simpler unsubstituted phenols, the reaction is governed by their Bronsted Leaving Group ability. On the other hand, the byproducts of the cage vary with these phenols. For the more acidic phenols the cage byproduct follows the Favorskii rearrangement to formp-hydroxyphenylacetic acid whereas for the weaker phenols other reactions such as reduction and hydrolysis begin to emerge. When the photolysis is conducted in octa acid (OA) containers, non-Favorskii, unrearranged fragments of the cage and other byproducts arise.

Name: 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Field, T; Peterson, J; Ma, CC; Jagadesan, P; Da Silva, JP; Rubina, M; Ramamurthy, V; Givens, RS 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 2021.0 ORG LETT published article about ALPHA-AMINO-ACIDS; ENANTIOSELECTIVE SYNTHESIS; DIASTEREODIVERGENT ACCESS; DUAL CATALYSIS; SPIROKETALS; CONSTRUCTION; GOLD in [Wang, Hongkai; Zeng, Tianlong; Chang, Weixing; Liu, Lingyan; Li, Jing] Nankai Univ, Coll Chem, State Key Lab, Tianjin 300071, Peoples R China; [Wang, Hongkai; Zeng, Tianlong; Chang, Weixing; Liu, Lingyan; Li, Jing] Nankai Univ, Coll Chem, Inst Elementoorgan Chem, Tianjin 300071, Peoples R China; [Li, Jing] Collaborat Innovat Ctr Chem Sci & Engn Tianjin, Tianjin 300071, Peoples R China in 2021.0, Cited 37.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5. COA of Formula: C8H8O2

An efficient catalytic asymmetric cascade cycloaddition reaction of arylalkynols with dioxopyrrolidines was developed. This reaction was achieved using Au(I) and (R)-BINOL-Ti(IV) bimetallic catalysts and exclusively delivered a series of chiral oxo-bridged bicyclic benzooxacine compounds in up to 86% yield with 96% ee as well as >33:1 dr. Meanwhile, three new s bonds and three new stereogenic centers were formed in a one-pot process.

About 4-Methoxybenzaldehyde, If you have any questions, you can contact Wang, HK; Zeng, TL; Chang, WX; Liu, LY; Li, J or concate me.. COA of Formula: C8H8O2

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

COA of Formula: C8H8O2. Yan, X; Yi, CW; Wang, YH; Cao, WD; Mao, DN; Ou, QQ; Shen, PY; Wang, HJ in [Yan, Xin; Yi, Chengwu; Wang, Yonghui; Cao, Wudi; Mao, Danni; Ou, Qingqing; Shen, Peiyao; Wang, Huijuan] Jiangsu Univ, Sch Environm & Safety Engn, Zhenjiang 212013, Jiangsu, Peoples R China published Multi-catalysis of nano-zinc oxide for bisphenol A degradation in a dielectric barrier discharge plasma system: Effect and mechanism in 2020.0, Cited 28.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

As a widely used chemical material, bisphenol A (BPA) is often used to produce kinds of chemicals, which lead risk to the ecological environment and human health. Based on the multi-catalysis of the nano-ZnO and multi-effect (chemical and physical) formed in the dielectric barrier discharge plasma (DBDP) system, the synergistic elimination of the BPA in the DBDP system combined with nano-ZnO was evaluated. The obtained experimental results showed that the superior adding amount of the nano-ZnO was 50 mg/L and the synergistic system on the condition had the best effect for the BPA degradation (85.4%), which was 17% higher than that in the sole DBDP system. When O-2 was bubbled into the reaction system, the degradation efficiency of the BPA in the synergistic system reached 100% after 20 min treatment. Compared with the alkaline solution, the acidic and weakly acidic solution could obtain higher treatment efficiency. (OH)-O-center dot and O-2(-) had a vital role for the BPA elimination in the synergistic system. The intermediate products detected by LC-MS included 4-cumylphenol, 4-isopropenylphenol, 4-tert-butylphenol, propiophenone, 1-(4-hydroxyphenyl) ethanone, tert-butylbenzene, benzoquinone and 1, 4-dihydroxybenzene.

About 4′-Hydroxyacetophenone, If you have any questions, you can contact Yan, X; Yi, CW; Wang, YH; Cao, WD; Mao, DN; Ou, QQ; Shen, PY; Wang, HJ or concate me.. COA of Formula: C8H8O2

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

Product Details of 123-11-5. Authors Yang, HF; Lu, SN; Chen, ZK; Wu, XF in AMER CHEMICAL SOC published article about in [Yang, Hefei; Lu, Shu-Ning; Chen, Zhengkai] Zhejiang Sci Tech Univ, Dept Chem, Hangzhou 310018, Peoples R China; [Wu, Xiao-Feng] Chinese Acad Sci, Dalian Inst Chem Phys, Dalian Natl Lab Clean Energy, Dalian 116023, Liaoning, Peoples R China; [Wu, Xiao-Feng] Univ Rostock, Leibniz Inst Katalyse eV, D-18059 Rostock, Germany in 2021.0, Cited 58.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

A silver-mediated [3 + 2] cycloaddition of azomethine ylides with trifluoroacetimidoyl chlorides for the rapid assembly of 5-(trifluoromethyl)imidazoles has been developed. Notable features of the reaction include readily accessible reagents, a broad substrate scope, and high efficiency. The protocol can be successfully applied to construct the analogue of the specific allosteric modulator of GABA(A) receptors. The silver species could be recycled by a simple operation.

Product Details of 123-11-5. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Yang, HF; Lu, SN; Chen, ZK; Wu, XF 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

Ammazzalorso, A; Gallorini, M; Fantacuzzi, M; Gambacorta, N; De Filippis, B; Giampietro, L; Maccallini, C; Nicolotti, O; Cataldi, A; Amoroso, R in [Ammazzalorso, Alessandra; Fantacuzzi, Marialuigia; De Filippis, Barbara; Giampietro, Letizia; Maccallini, Cristina; Amoroso, Rosa] Univ G dAnnunzio, Dept Pharm, Unit Med Chem, Chieti, Italy; [Gallorini, Marialucia; Cataldi, Amelia] Univ G dAnnunzio, Dept Pharm, Unit Anat, Chieti, Italy; [Gambacorta, Nicola; Nicolotti, Orazio] A Moro Univ, Dept Farm Sci Farmaco, Unit Med Chem, Bari, Italy published Design, synthesis and biological evaluation of imidazole and triazole-based carbamates as novel aromatase inhibitors in 2021.0, Cited 33.0. Name: Mequinol. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5.

In the search for novel aromatase inhibitors, a series of triazole and imidazole-based carbamate derivatives were designed and synthesized. Final compounds were thus evaluated against human aromatase by in vitro kinetic experiments in a fluorimetric assay in comparison with letrozole. The effect of most active derivatives 13a and 15c was then evaluated in vitro on the human breast cancer cell line MCF7 by MTT assay, cytotoxicity assay (LDH release) and cell cycle analysis, revealing a dose-dependent inhibition profile of cell viability and low micromolar IC50 values. In addition, docking simulations were also carried out to elucidate at a molecular level of detail the binding modes adopted to target human aromatase. (C) 2020 Elsevier Masson SAS. All rights reserved.

About Mequinol, If you have any questions, you can contact Ammazzalorso, A; Gallorini, M; Fantacuzzi, M; Gambacorta, N; De Filippis, B; Giampietro, L; Maccallini, C; Nicolotti, O; Cataldi, A; Amoroso, R or concate me.. Name: Mequinol

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