- An efficient synthesis of novel di-heterocyclic benzazole derivatives and evaluation of their antiproliferative activities
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A series of unsymmetrical nine di-heterocyclic compounds of benzazole derivatives were synthesized at one step via cyclization reaction. The compounds evaluated for in?vitro cytotoxic activity against A549, A498, HeLa, and HepG2 cancer cell lines. The biological evaluation results show that 23, 26 and 29 exhibit better activity against HepG2 and HeLa cancer cell lines. Compound 23 also showed good activity against A549, and A498 cancer cell lines. The analogs were further performed molecular docking studies against human cytochrome P450 2C8 monooxygenase enzyme, calculated some theoretical quantum parameters, ADMET descriptor and molecular electrostatic potential analysis. The strategy applied in this research work may act as a perspective for the rational design of potential anticancer drugs. Communicated by Ramaswamy H. Sarma.
- Algul, Oztekin,Ersan, Ronak Haj,Alagoz, Mehmet Abdullah,Duran, Nizami,Burmaoglu, Serdar
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p. 6926 - 6938
(2020/08/13)
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- Regio- and diastereoselective decarboxylative coupling of heteroaromatic alkanes
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Allylic esters of heteroaromatic alkanes undergo facile palladium-catalyzed decarboxylative coupling. The resulting C-C bond is formed with high diastereoselectivity and high regioselectivity for coupling at the more substituted allyl terminus. It is proposed that this unusual combination of selectivities results from a tandem allylation/aza-Cope rearrangement sequence. After allylation, decarboxylative dearomatization produces an intermediate for the aza-Cope rearrangement. The subsequent aza-Cope rearrangement occurs under mild conditions because it is driven by rearomatization. Copyright
- Waetzig, Shelli R.,Tunge, Jon A.
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p. 4138 - 4139
(2008/01/27)
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