Day: December 8, 2021

Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS in [Aly, Ashraf A.; El-Sheref, Essmat M.; Bakheet, Momtaz E. M.; Ibrahim, Mahmoud A. A.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Mourad, Mai A. E.] Port Said Univ, Med Chem Dept, Fac Pharm, Port Said 42526, Egypt; [Kaoud, Tamer S.] Menia Univ, Fac Pharm, Dept Med Chem, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Brase, Stefan] Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Nieger, Martin] Univ Helsinki, Dept Chem, POB 55, Helsinki 00014, Finland; [Garvalov, Boyan K.] Mannhe Univ Heidelberg, Ctr Biomed & Med Technol Mannheim, Med Fac, D-68167 Mannheim, Germany; [Dalby, Kevin N.; Kaoud, Tamer S.] Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA published Design, synthesis and biological evaluation of fused naphthofuro[3,2-c]quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma in 2019, Cited 57. COA of Formula: C9H7NO2. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

Approximately 60% of human cancers exhibit enhanced activity of ERK1 and ERK2, reflecting their multiple roles in tumor initiation and progression. Acquired drug resistance, especially mechanisms associated with the reactivation of the MAPK (RAF/MEK/ERK) pathway represent a major challenge to current treatments of melanoma and several other cancers. Recently, targeting ERK has evolved as a potentially attractive strategy to overcome this resistance. Herein, we report the design and synthesis of novel series of fused naphthofuro[3,2-c] quinoline-6,7,12-triones 3a-f and pyrano[3,2-c]quinoline-6,7,8,13-tetraones 5a,b and 6, as potential ERK inhibitors. New inhibitors were synthesized and identified by different spectroscopic techniques and X-ray crystallography. They were evaluated for their ability to inhibit ERK1/2 in an in vitro radioactive kinase assay. 3b and 6 inhibited ERK1 with IC50s of 0.5 and 0.19 mu M, and inhibited ERK2 with IC50s of 0.6 and 0.16 mu M respectively. Kinetic mechanism studies revealed that the inhibitors are ATP-competitive inhibitors where 6 inhibited ERK2 with a K-i of 0.09 mu M. Six of the new inhibitors were tested for their in vitro anticancer activity against the NCI-60 panel of tumor cell lines. Compound 3b and 6 were the most potent against most of the human tumor cell lines tested. Moreover, 3b and 6 inhibited the proliferation of the BRAF mutant A375 melanoma cells with IC50s of 3.7 and 0.13 mu M, respectively. In addition, they suppressed anchorage-dependent colony formation. Treatment of the A375 cell line with 3b and 6 inhibited the phosphorylation of ERK substrates p-90RSK and ELK-1 and induced apoptosis in a dose dependent manner. Finally, a molecular docking study showed the potential binding mode of 3b and 6 within the ATP catalytic binding site of ERK2.

COA of Formula: C9H7NO2. Bye, fridends, I hope you can learn more about C9H7NO2, If you have any questions, you can browse other blog as well. See you lster.

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 Agriculture; Chemistry; Food Science & Technology very interesting. Saw the article Synthesis of Three Bioactive Aromatic Compounds by Introducing Polyketide Synthase Genes into Engineered Escherichia coli published in 2019. SDS of cas: 86-95-3, Reprint Addresses Ahn, JH (corresponding author), Konkuk Univ, Bio Mol Informat Ctr, Dept Biosci & Biotechnol, Seoul 05029, South Korea.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one

Intermediates in aromatic amino acid biosynthesis can serve as substrates for the synthesis of bioactive compounds. In this study we used two intermediates in the shikimate pathway of Escherichia coli, chorismate and anthranilate, to synthesize three bioactive compounds: 4-hydroxycoumarin (4-HC), 2,4-dihydroxyquinoline (DHQ), and 4-hydroxy-1-methyl-2(1H)-quinolone (NMQ). We introduced genes for the synthesis of salicylic acid from chorismate to supply the substrate for 4-HC and the gene encoding N-methyltransferase for the synthesis of N-methylanthranilate from anthranilate. Polyketide synthases and coenzyme (Co)A ligases were tested to determine the optimal combination of genes for the synthesis of each compound. We also tested several constructs and identified the best one for increasing levels of endogenous substrates for chorismate, anthranilate, and malonyl-CoA. With the use of these strategies, 255.4 mg/L 4-HC, 753.7 mg/L DHQ, and 17.5 mg/L NMQwere synthesized. This work provides a basis for the synthesis of diverse coumarin and quinoline derivatives with potential medical applications.

SDS of cas: 86-95-3. Welcome to talk about 86-95-3, If you have any questions, you can contact Choo, HJ; Ahn, JH or send Email.

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. Authors Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H in AMER CHEMICAL SOC published article about in [Kummer, David A.] Lundbeck La Jolla Res Ctr Inc, San Diego, CA 92121 USA; [Chheda, Pratik R.; Nishimura, Rachel T.; McClure, Kelly J.; Venkatesan, Hariharan] Janssen Res & Dev, Discovery Chem, San Diego, CA 92121 USA in 2021, Cited 63. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

A one-pot, Hantzsch ester-mediated Knoevenagel condensation-reduction reaction has been developed for alkylation of a wide range of substituted 2,4-quinoline diols and 2,4-pyridine diols with aldehydes. The process is operationally simple to perform, scalable, and provides highly useful C-3 alkylated quinoline and pyridine diols in yields of 58-92%. The alkylation products can be converted to 2,4-dihaloquinoline and pyridine substrates for further functionalization.

Category: indole-building-block. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Chheda, PR; Kummer, DA; Nishimura, RT; McClure, KJ; Venkatesan, H 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

SDS of cas: 99-93-4. Yang, S; Xiong, MF; Tian, WQ; Zhang, H; Xiao, XY; Liu, HY; Chang, CK in [Yang, Shuang; Xiong, Ming-Feng; Tian, Wan-Qun; Zhang, Hao; Xiao, Xin-Yan; Liu, Hai-Yang] South China Univ Technol, Dept Chem, Key Lab Funct Mol Engn Guangdong Prov, Guangzhou 510641, Peoples R China; [Chang, Chi-Kwong] Michigan State Univ, Dept Chem, E Lansing, MI 48824 USA published Construction of C-O bond via cross-dehydrogenative coupling of sp [3] C-H bond with phenols catalyzed by copper porphyrin in 2020, Cited 42. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

Copper porphyrin-catalyzed construction of ether bond by cross-dehydrogenative coupling of sp [3] C-H bond with phenols bearing electron-withdrawing groups (EWG) was described for the first time. A broad range of substrates afforded different acetals in moderate to excellent yields with good functional group tolerance. The developed method is not only suitable for phenol substrates with ortho-directing groups, but also suitable for those phenol without ortho-directing groups. Significantly, a high turnover number (TON) up to 7300 was achieved in gram-level test. (C) 2020 Elsevier Ltd. All rights reserved.

Welcome to talk about 99-93-4, If you have any questions, you can contact Yang, S; Xiong, MF; Tian, WQ; Zhang, H; Xiao, XY; Liu, HY; Chang, CK or send Email.. SDS of cas: 99-93-4

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

Sheet, D; Bera, A; Jana, RD; Paine, TK in [Sheet, Debobrata; Bera, Abhijit; Jana, Rahul Dev; Paine, Tapan Kanti] Indian Assoc Cultivat Sci, Sch Chem Sci, 2A & 2B Raja SC Mullick Rd, Kolkata 700032, India; [Sheet, Debobrata] Presidency Univ, Dept Chem, 86-1 Coll St, Kolkata 700073, India published Oxidizing Ability of a Dioxygen-Activating Nonheme Iron(II)-Benzilate Complex Immobilized on Gold Nanoparticles in 2019.0, Cited 74.0. SDS of cas: 100-51-6. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

An iron(II)-benzilate complex [(TPASH)Fe-II(benzilate)]ClO4@C8Au (2) (TPASH = 11-((6-((bis(pyridin-2-ylmethyl)amino)methyl)pyridin-2-yl)methoxy)undecane-1-thiol) immobilized on octanethiol stabilized gold nanoparticles (C8Au) of core diameter less than 5 nm has been prepared to evaluate its reactivity toward O-2-dependent oxidations compared to a nonimmobilized complex [(TPA-O-Allyl)Fe-II(benzilate)]ClO4 (1a) (TPA-O-Allyl = N-(6-(allyloxymethyl)pyridin-2-yl)methyl)(pyridin-2-yl)-N-(pyridin-2-ylmethyl)methanamine). X-ray crystal structure of the nonimmobilized complex la reveals a six-coordinate iron(II) center in which the TPA-O-Allyl acts as a pentadentate ligand and the benzilate anion binds in monodentate fashion. Both the complexes (1a and 2) react with dioxygen under ambient conditions to form benzophenone as the sole product through decarboxylation of the coordinated benzilate. Interception studies reveal that a nucleophilic iron-oxygen intermediate is formed in the decarboxylation reaction. The oxidants from both the complexes are able to carry out oxo atom transfer reactions. The immobilized complex 2 not only performs faster decarboxylation but also exhibits enhanced reactivity in oxo atom transfer to sulfides. Importantly, the immobilized complex 2, unlike 1a, displays catalytic turnovers in sulfide oxidation. However, the complexes are not efficient to carry out cis-dihydroxylation of alkenes. Although the immobilized complex yields a slightly higher amount of cis-diol from 1-octene, restricted access of dioxygen and substrates at the coordinatively saturated metal centers of the complexes likely makes the resulting iron-oxygen species less active in oxygen atom transfer to alkenes. The results implicate that surface immobilized nonheme iron complexes containing accessible coordination sites would exhibit better reactivity in O-2-dependent oxygenation reactions.

SDS of cas: 100-51-6. About Benzyl Alcohol, If you have any questions, you can contact Sheet, D; Bera, A; Jana, RD; Paine, TK 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

COA of Formula: C9H10O3. Authors Kulkarni, MR; Lad, NP; Khedkar, VM; Gaikwad, ND in WILEY published article about in [Kulkarni, Mahesh R.; Lad, Nitin P.; Gaikwad, Nitin D.] KRT Arts BH Commerce & AM Sci Coll, Dept Chem, Organ Chem Res Ctr, Gangapur Rd, Nasik 422002, India; [Khedkar, Vijay M.] Vishwakarma Univ, Sch Pharm, Pune, Maharashtra, India in 2021.0, Cited 22.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

With the aim of expanding the scope of SAR on piperlongumine (PL), a naturally occurring anticancer molecule, we have designed a novel hybrid molecule bearing 3,4-dihydroisoquinolin-1(2H)-one and trans-cinnamic acids. The structure, based on hybridization strategy, is used for hybridization of naturally occurring scaffolds. We have synthesized 14 hybrid molecules by coupling 3,4-dihydroisoquinolin-1(2H)-one core with cinnamic acids using the mix anhydride approach. The newly synthesized inhibitors were evaluated for cell viability against breast cancer MCF-7 and cervical cancer HeLa cell lines. Furthermore, the active compounds were screened for their potential in breast cancer MDA-MB-231, cervical cancer C33A cell lines, prostate cancer DU-145, PC-3, and normal VERO cells. From the series, compound 10g was seen to inhibit MCF-7 cell growth significantly with GI(50) < 0.1 mu M along with growth inhibition in MDA-MB-231 (GI(50) = 20 mu M) and C33A (GI(50) = 3.2 mu M). While the inhibitor 10i inhibits MCF-7 breast cancer cell growth GI(50) = 3.42 mu M along with inhibition of cell growth in MDA-MB-231 (GI(50) = 30 mu M), HeLa (GI(50) = 7.67 mu M), C33A (GI(50) = 13 mu M), DU-145 (GI(50) = 6.45 mu M), PC-3 (GI(50) = 8.68 mu M), and VERO (GI(50) = 2.93 mu M), respectively. Furthermore, molecular docking study demonstrated these compounds could bind tightly to the colchicine domain of tubulin through a network of favorable steric and electrostatic interactions and thus act as a tubulin polymerization inhibitor. Welcome to talk about 120-14-9, If you have any questions, you can contact Kulkarni, MR; Lad, NP; Khedkar, VM; Gaikwad, ND or send Email.. COA of Formula: C9H10O3

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. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Novel 1,2,4-oxadiazole-chalcone/oxime hybrids as potential antibacterial DNA gyrase inhibitors: Design, synthesis, ADMET prediction and molecular docking study published in 2021.0, Reprint Addresses Ibrahim, TS (corresponding author), King Abdulaziz Univ, Fac Pharm, Dept Pharmaceut Chem, Jeddah 21589, Saudi Arabia.; Mohamed, MFA (corresponding author), Sohag Univ, Fac Pharm, Dept Pharmaceut Chem, Sohag 82524, Egypt.. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde.

New antibacterial drugs are urgently needed to tackle the rapid rise in multi-drug resistant bacteria. DNA gyrase is a validated target for the development of new antibacterial drugs. Thus, in the present investigation, a novel series of 1,2,4-oxadiazole-chalcone/oxime (6a-f) and (7a-f) were synthesized and characterized by IR, NMR (1H and 13C) and elemental analyses. The title compounds were evaluated for their in-vitro antimicrobial activity by the modified agar diffusion method as well as their E. coli DNA gyrase inhibitory activity. The minimum inhibitory concentration (MIC) and the structure activity relationships (SARs) were evaluated. Among all, compounds 6a, 6c-e, 7b and 7e were the most potent and proved to possess broad spectrum activity against the tested Gram-positive and Gram-negative organisms. Additionally, compounds 6a (against S. aureus), 6c (against B. subtilis and E. hirae), 6e (against E. hirae), 6f, 7a and 7c (against E. coli) and 7d (against B. subtilis), with MIC value of 3.12 mu M were two-fold more potent than the standard ciprofloxacin (MIC = 6.25 mu M). Mechanistically, compounds 6c, 7c, 7e and 7b had good inhibitory activity against E. coli gyrase with IC50 values of 17.05, 13.4, 16.9, and 19.6 mu M, respectively, in comparison with novobiocin (IC50 = 12.3 mu M) and ciprofloxacin (IC50 = 10.5 mu M). The molecular docking results at DNA gyrase active site revealed that the most potent compounds 6c and 7c have binding mode and docking scores comparable to that of ciprofloxacin and novobiocin suggesting their antibacterial activity via inhibition of DNA gyrase. Finally, the predicted parameters of Lipinski’s rule of five and ADMET analysis showed that 6c and 7c had good drug-likeness and acceptable physicochemical properties. Therefore, the hybridization of the chalcone and oxadiazole moieties could be promising lead as antibacterial candidate which merit further future structural optimizations.

Welcome to talk about 123-11-5, If you have any questions, you can contact Ibrahim, TS; Almalki, AJ; Moustafa, AH; Allam, RM; Abuo-Rahma, GEDA; El Subbagh, HI; Mohamed, MFA or send Email.. Product Details of 123-11-5

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

Product Details of 100-51-6. Singh, R; Ryu, I; Yadav, H; Park, J; Jo, JW; Yim, S; Lee, JJ in [Singh, Ranbir; Ryu, Ilhwan; Yadav, Hemraj; Park, Jongdeok; Jo, Jea Woong; Lee, Jae-Joon] Dongguk Univ, Res Ctr Photoenergy Harvesting & Convers Technol, Dept Energy Mat & Engn, Seoul 04620, South Korea; [Yim, Sanggyu] Kookmin Univ, Dept Chem, Seoul 02707, South Korea published Non-hydrolytic sol-gel route to synthesize TiO2 nanoparticles under ambient condition for highly efficient and stable perovskite solar cells in 2019.0, Cited 46.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

For developing low-temperature processed electron-transporting layer in perovskite solar cells, titanium oxide (TiO2) nanoparticle was synthesized through the non-hydrolytic sol-gel route. TiO2 nanoparticles showed uniform film coverage, high transparency in the visible region with wide optical bandgap, and high electrical conductivity after systematically optimizing the synthetic reaction time, the thermal annealing temperature, and the concentration of Nb doping. When TiO2 nanoparticle was introduced as an electron-transporting layer through low-temperature deposition process, the perovskite solar cells fabricated in ambient conditions showed high efficiencies of 18.97% and 13.51% on the rigid glass and the flexible plastic substrate, respectively. An impressively high open circuit voltage of 1.17 V and short circuit current density of 22.21 mA cm(-2) were achieved due to the well aligned work function and better electrical conductivity of Nb-doped LT-TiO2 layer. Importantly, solar cells fabricated with TiO2 nanoparticle showed high thermal stability, negligible hysteresis, and reduced charge recombination loss at electron-transporting layer/perovskite interfaces. This study shows that TiO2 nanoparticle can be obtained through the low cost and facile synthesis and has high potential as an electron-transporting layer for low-temperature processable perovskite solar cells.

Welcome to talk about 100-51-6, If you have any questions, you can contact Singh, R; Ryu, I; Yadav, H; Park, J; Jo, JW; Yim, S; Lee, JJ or send Email.. Product Details of 100-51-6

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 Sequential Functionalization of meta-C-H and ipso-C-O Bonds of Phenols WOS:000458348300019 published article about NICKEL-CATALYZED AMINATION; ARYL 2-PYRIDYL ETHERS; ARENES; ACTIVATION; BORYLATION; OLEFINATION; ARYLATION; LIGAND; ALKYLATION; CLEAVAGE in [Xu, Jiancong; Chen, Jingjing; Gao, Feng; Xie, Shuguang; Xu, Xiaohua; Jin, Zhong] Nankai Univ, Coll Chem, State Key Lab, Tianjin 300071, Peoples R China; [Xu, Jiancong; Chen, Jingjing; Gao, Feng; Xie, Shuguang; Xu, Xiaohua; Jin, Zhong] Nankai Univ, Coll Chem, Inst Elementoorgan Chem, Tianjin 300071, Peoples R China; [Xu, Xiaohua; Jin, Zhong] Collaborat Innovat Ctr Chem Sci & Engn Tianjin, Tianjin 300071, Peoples R China; [Yu, Jin-Quan] Scripps Res Inst, Dept Chem, 10550 North Torrey Pines Rd, La Jolla, CA 92037 USA in 2019, Cited 48. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6. Application In Synthesis of m-Methoxyphenol

The use of a template as a linchpin motif in directed remote C-H functionalization is a versatile yet relatively underexplored strategy. We have developed a template-directed approach to realizing one-pot sequential palladium-catalyzed meta-selective C-H olefination of phenols, and nickel-catalyzed ipso-C-O activation and arylation. Thus, this bifunctional template converts phenols to synthetically useful 1,3-disubstituted arenes.

Bye, fridends, I hope you can learn more about C7H8O2, If you have any questions, you can browse other blog as well. See you lster.. Application In Synthesis of m-Methoxyphenol

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 Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article 3,7-bis-benzylidene hydrazide ciprofloxacin derivatives as promising antiproliferative dual TOP I & TOP II isomerases inhibitors published in 2021. Category: indole-building-block, Reprint Addresses Abdel-Aziz, M (corresponding author), Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt.; Abuo-Rahma, GEDA (corresponding author), Deraya Univ, Fac Pharm, Dept Pharmaceut Chem, New Minia, Minia, Egypt.. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde

We report herein design and synthesis of a new series of 3,7-bis-benzylidenes of ciprofloxacin. Most of the target compounds revealed good cytotoxic activity; the most potent 4e and 4i achieved strong broad spectrum antiproliferative activity with comparable activity to Doxorubicin with IC50 (M-mu) of 1.21 +/- 0.02, 0.87 +/- 0.04, 1.21 +/- 0.02; 0.41 +/- 0.02, 0.57 +/- 0.06, 1.31 +/- 0.04 and 1.26 +/- 0.01, 1.79 +/- 0.04, 0.63 +/- 0.01 against leukemia cancer cell line HL-60 (TB), colon cancer cell line HCT-116 and breast cancer cell line MCF7, respectively. Moreover, the most potent derivative 4i induced apoptosis at G2/M phase Investigating the mechanism of action of compounds 4e, 4 h and 4i exhibited promising dual TOP I alpha and TOP IIB % inhibition comparable to Camptothecin and Etoposide; respectively. Docking of 4e, 4 h and 4i into the active site of topo I and II proteins compared to Camptothein and Etoposide revealed acceptable binding score and augmented enzyme assay data. Hence, 4e and 4i are promising targeted antiproliferative dual acting TOP I alpha TOP IIB inhibitors that require further optimization.

Welcome to talk about 120-14-9, If you have any questions, you can contact Samir, M; Ramadan, M; Abdelrahman, MH; Abdelbaset, MS; Abourehab, MAS; Abdel-Aziz, M; Abuo-Rahma, GEDA or send Email.. 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