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Synthesis and anticancer evaluation of some new pyrazolo[3,4‐d][1,2,3]triazin‐4‐ones, pyrazolo[1,5‐a]pyrimidines, and imidazo[1,2‐b]pyrazoles clubbed with carbazole
Journal of Heterocyclic Chemistry ( IF 2.4 ) Pub Date : 2020-09-13 , DOI: 10.1002/jhet.4148
Samir Bondock 1, 2 , Salwa Alqahtani 3 , Ahmed M. Fouda 1
Affiliation  

Carbazole represents as a promising template for cancer treatment as it exists in the skeleton of numerous man‐made and natural anticancer agents. In this regard, new sets of novel functionalized pyrazolo[3,4‐d][1,2,3]triazin‐4‐ones 6a‐e and 10a‐e, pyrazolo[1,5‐a]pyrimidines 16a,b and imidazo[1,2‐b]pyrazoles 20a,b and 23a‐c having carbazole moiety were efficiently synthesized, characterized, and mechanistically discussed. They were also evaluated against three human cancer cell lines (HCT‐116, HepG‐2, and MCF‐7) and one standard human cell line (REP1) for their in vitro anticancer activity. The results declared that seven compounds 10d, 10e, 12b, 12d, 12e, 16a, and 23a had potent anticancer activity, having IC50 values in the range 2.97 to 10.31 μM. The most effective compounds 10d and 10e inhibited the growth of all screened cancer cell lines and did not reveal human toxicity.

中文翻译:

一些新型吡唑并[3,4-d] [1,2,3]三嗪-4-酮,吡唑并[1,5-a]嘧啶和咪唑并[1,2-b]吡唑类化合物的合成和抗癌性评估咔唑

咔唑代表着许多有希望的模板,因为它存在于许多人造和天然抗癌药物的骨架中。在这方面,新的一组新颖的功能化吡唑并[3,4- d ] [1,2,3]三嗪-4-酮6a-e10a-e,吡唑并[1,5- a ]嘧啶16a,b和咪唑并[1,2- b ]吡唑20a,b23a-c具有咔唑部分的具有高效率的合成,表征和机理讨论。还针对三种人类癌细胞系(HCT-116,HepG-2和MCF-7)和一种标准人类细胞系(REP1)评估了它们的体外抗癌活性。结果表明,七个化合物10d10e12b12d12e16a23a具有有效的抗癌活性,IC 50值在2.97至10.31μM范围内。最有效的化合物10d10e抑制所有筛选的癌细胞系的生长,并且没有显示出人类毒性。
更新日期:2020-09-13
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