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Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines.

ABSTRACT: Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms of antiproliferative efficacy with GI50 values in the range of 0.296 to 250 ?M. Molecular docking studies indicated that Compounds 8a and 11c are accommodated in the colchicine binding site of tubulin in two different ways.

SUBMITTER: Al Matarneh CM

PROVIDER: S-EPMC7036904 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines.

Al Matarneh Cristina Maria CM Amarandi Roxana Maria RM Craciun Anda Mihaela AM Mangalagiu Ionel I II Zbancioc Gheorghita G Danac Ramona R

Molecules (Basel, Switzerland) 20200125 3

Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds 8a and 11c) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound 11c showed a broad spectrum in terms ...[more]

PMID: 31991806

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