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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
Author(s) -
Bondock Samir,
Alqahtani Salwa,
Fouda Ahmed M.
Publication year - 2021
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.4148
Subject(s) - chemistry , moiety , carbazole , stereochemistry , cell culture , in vitro , cancer cell lines , cancer cell , cancer , combinatorial chemistry , biochemistry , organic chemistry , genetics , biology
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 IC 50 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.