title: Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds.
abstract: A series of chalcone analogous compounds were designed and synthesized. Replacing/substituting the enone or ethylenic bridge of the parent chalcone with rigid heterocyclic moieties or substituted aromatic amines gave nineteen target compounds. Their cytotoxic activities were screened against both breast and liver cancer cells as well as breast and liver normal cells. Target compounds were also evaluated for their inhibition activity of tubulin beta polymerization. Target compound 2e, 3a, 3b, 3c, 4a-4d, 5a, 5b and 6 showed broad spectrum excellent anticancer activity against both MCF-7 and HepG2. Compound 4a showed the most TUBb inhibition activity.
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11561, Cairo, Egypt.
authors.forename: S
authors.initials: S
authors.lastname: El-Meligie
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11561, Cairo, Egypt; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt.
authors.forename: Azza T
authors.initials: AT
authors.lastname: Taher
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11561, Cairo, Egypt. Electronic address: Aliaa.kamal@pharma.cu.edu.eg.
authors.forename: Aliaa M
authors.initials: AM
authors.lastname: Kamal
authors.affiliation: Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt.
authors.forename: A
authors.initials: A
authors.lastname: Youssef
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D001940:Breast / Q000166:cytology; D049109:Cell Proliferation / Q000187:drug effects; D002599:Chalcone / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D056945:Hep G2 Cells; D006801:Humans; D008099:Liver / Q000166:cytology; D061986:MCF-7 Cells; D014404:Tubulin / Q000737:chemistry; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000970:Antineoplastic Agents; D014404:Tubulin; D050257:Tubulin Modulators; D002599:Chalcone
keywords: Cancer cell lines; Chalcone derivatives; Cytotoxic activity; Normal cell lines; Replacing enone bridge; Tubulin beta polymerization inhibitors