title: Facile synthesis and antiproliferative activity of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines.
abstract: A series of 7H-benzo[7,8]chromeno[2,3-d]pyrimidin-8-amines 6a-t were synthesized as new potential antiproliferative agents. The in vitro antiproliferative activity evaluation of title compounds using MTT assay revealed that most compounds showed significant activity against tested cancer cell lines (A549, MOLT-4, and HeLa). The 2-fluoro-aniline derivatives 6e and 6l were the most active compounds against A549 and MOLT-4 cells, respectively. The benzylamine analog 6h showed superior activity against HeLa cells. However, compound 6l with IC50values of 5.2-6.9 μM had the best profile of activity against all tested cell lines. The morphological and flow cytometric analyses showed that compound 6l can induce apoptosis in the MOLT-4 cells.
authors.affiliation: Department of Chemistry, College of Science, Yazd University, Yazd, PO Box 8915813149, Iran.
authors.forename: Hamidreza
authors.initials: H
authors.lastname: Akrami
authors.affiliation: Department of Biotechnology, Iranian Research Organization for Science and Technology (IROST), Tehran, Iran.
authors.forename: Maliheh
authors.initials: M
authors.lastname: Safavi
authors.affiliation: Department of Chemistry, College of Science, Yazd University, Yazd, PO Box 8915813149, Iran.
authors.forename: Bibi Fatemeh
authors.initials: BF
authors.lastname: Mirjalili
authors.affiliation: Department of Biology, Ashkezar Branch, Islamic Azad University, Ashkezar, Iran.
authors.forename: Mahmood
authors.initials: M
authors.lastname: Dehghani Ashkezari
authors.affiliation: Department of Biology, Ashkezar Branch, Islamic Azad University, Ashkezar, Iran.
authors.forename: Farhang
authors.initials: F
authors.lastname: Dadfar
authors.affiliation: Department of Chemistry, College of Science, Yazd University, Yazd, PO Box 8915813149, Iran.
authors.forename: Najme
authors.initials: N
authors.lastname: Mohaghegh
authors.affiliation: Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
authors.forename: Saeed
authors.initials: S
authors.lastname: Emami
authors.affiliation: Institute of Biochemistry and Biophysics, Department of Biochemistry, University of Tehran, Tehran, Iran.
authors.forename: Fahimeh
authors.initials: F
authors.lastname: Salehi
authors.affiliation: Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.
authors.forename: Hamid
authors.initials: H
authors.lastname: Nadri
authors.affiliation: Institute of Biochemistry and Biophysics, Department of Biochemistry, University of Tehran, Tehran, Iran.
authors.forename: Sussan K
authors.initials: SK
authors.lastname: Ardestani
authors.affiliation: Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Loghman
authors.initials: L
authors.lastname: Firoozpour
authors.affiliation: Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran; Department of Pharmaceutical Biomaterials and Medical Biomaterials Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. Electronic address: khoobi@tums.ac.ir.
authors.forename: Mehdi
authors.initials: M
authors.lastname: Khoobi
authors.affiliation: Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran; Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran. Electronic address: aforoumadi@yahoo.com.
authors.forename: Alireza
authors.initials: A
authors.lastname: Foroumadi
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011743:Pyrimidines
keywords: Anticancer; Benzochromene; Cytotoxic agents; Polycyclic compounds