Authors Noha, RM; Abdelhameid, MK; Ismail, MM; Mohammed, MR; Salwa, E in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about BIOLOGICAL EVALUATION; CHROMOSOME INSTABILITY; TOPOISOMERASE-I; DERIVATIVES; TUBULIN; APOPTOSIS; DEFECTS; CRYSTAL; ANALOGS; VITRO in [Noha, Ryad M.; Ismail, M. Mohsen] Misr Univ Sci & Technol, Coll Pharmaceut Sci & Drug Mfg, Pharmaceut Organ Chem Dept, POB 77, Giza, Egypt; [Abdelhameid, Mohammed K.; Ismail, M. Mohsen; Salwa, Elmeligie] Cairo Univ, Fac Pharm, Pharmaceut Organ Chem Dept, Cairo 11561, Egypt; [Mohammed, Manal R.] Natl Ctr Radiat Res & Technol, Dept Radiat Biol, Cairo 11787, Egypt; [Abdelhameid, Mohammed K.] 33 Kasr El Aini St, Cairo, Egypt in 2021, Cited 39. Recommanded Product: 4-Methoxybenzaldehyde. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
A novel series of benzimidazole derivatives with methoxylated aryl groups was designed and synthesized as molecules with potential cytotoxic activity. In vitro cytotoxic activity over HCT-116 cells showed that N-(benzimidazothiazolone)acetamides 11a, 11b and 11c were found to be the most cytotoxic compounds compared camptothecin (CPT). The tested compounds had a dual topoisomerase I-beta (Topo I-beta) and tubulin inhibiting activities when compared to CPT and Podophyllotoxin (Podo) where, compounds l0a, l0b, 11a and 11b exhibited a potent inhibitory activity on Topo I-b enzyme in nano-molar concentration, on the other hand, compounds 12b and 13b exhibited the best inhibitory activity beta-tubulin polymerization. Results of the cell cycle analysis as well as the results of annexin-V on HCT-116 cells showed that benzimidazothiazoles 12b and 13b had a pro-apoptotic activity higher than CPT by 1.33- and 1.30-folds, respectively. Moreover, the concentration of p53, Bax/Bcl-2 ratio and caspase 3/7 increased in compounds l0b, 11b, l2b, 13b, especially, compounds 11b and 13b exhibited an increased level of these mediators than CPT. Finally, compound 11b regulated the radiosensitizing activity of the HCT-116 cells by modulating the chromosomal instability. (c) 2020 Elsevier Masson SAS. All rights reserved.
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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