title: Synthesis of novel amides based on acridone scaffold with interesting antineoplastic activity.
abstract: In search of novel cytotoxic agents based on acridone scaffold, twenty five derivatives of acridone-2- carboxamide were synthesized and evaluated against a panel of eleven cancer cell lines by using MTT assay. Amides, A5 and A8 (IC50 = 0.3 µM) exhibited good cytotoxicity against MCF7. Compound A22 (IC50 = 4.3 µM) was found to be selectively cytotoxic against cancer cell line MCF7 and KB403. Particularly, promising cytotoxic activities were shown by amides A6 (IC50 = 0.7 µM), A16 (IC50 = 6.3 µM), A8 (IC50 = 0.9 µM ), A21 (IC50 = 1.3 µM), A5 (IC50 = 2.9 µM), A8 (IC50 = 2.8 µM), A14 (IC50 = 0.8 µM), A9 (IC50 = 0.8 µM) and A8 (IC50 = 0.4 µM) against cell lines; PA1, WRL68, CaCO2, TK-10, K-562, PC-3, HOP-92, ECV-304 and UACC-257, respectively. The favorable cytotoxic profile and non-toxicity towards normal human cells displayed by the derivative revealed their potential for further anticancer drug developments.
authors.affiliation: Sinhgad Institute of Pharmacy, Narhe, Pune - 411041, affiliated to University of Pune, India. anand_mahajan@yahoo.com.
authors.forename: Anand A
authors.initials: AA
authors.lastname: Mahajan
authors.forename: Rajesh A
authors.initials: RA
authors.lastname: Rane
authors.forename: Anish A
authors.initials: AA
authors.lastname: Amritkar
authors.forename: Shital S
authors.initials: SS
authors.lastname: Naphade
authors.forename: Pankaj B
authors.initials: PB
authors.lastname: Miniyar
authors.forename: Pavan Kumar
authors.initials: PK
authors.lastname: Bangalore
authors.forename: Rajshekhar
authors.initials: R
authors.lastname: Karpoormath
mesh_terms: D000166:Acridines / Q000737:chemistry*; D054831:Acridones; D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; 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; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D000166:Acridines; D054831:Acridones; D000577:Amides; D000970:Antineoplastic Agents; C041300:acridone