title: Synthesis of novel carbazole chalcones as radical scavenger, antimicrobial and cancer chemopreventive agents.
abstract: A series of novel carbazole chalcones has been synthesised and evaluated for radical scavenging activity, cytotoxicity and antimicrobial activities. Compounds 12m, 12o and 12c exhibited good 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, compounds 12e, 12m and 12d were excellent hydroxyl radical scavengers and compounds 12a, 12e, 12g, 12n and 12m have shown inhibition of oxidative DNA damage induced by 2,2'-azobis (2-amidinopropane hydrochloride). Compounds 12j, 12i, 12n, 12c, 12m and 12e were most active against the selected cancer cell lines. Compounds 12a, 12e and 12m showed good antibacterial activity and compounds 12h and 12m have shown good antifungal activity. All the compounds were subjected for absorption, distribution, metabolism and excretion (ADME) predictions by computational method and found that these molecules could be considered as potential candidates for oral drug development.
authors.affiliation: Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University, Solapur, Maharashtra. bandgar_bp@yahoo.com
authors.forename: Babasaheb P
authors.initials: BP
authors.lastname: Bandgar
authors.forename: Laxman K
authors.initials: LK
authors.lastname: Adsul
authors.forename: Shrikant V
authors.initials: SV
authors.lastname: Lonikar
authors.forename: Hemant V
authors.initials: HV
authors.lastname: Chavan
authors.forename: Sadanand N
authors.initials: SN
authors.lastname: Shringare
authors.forename: Sachin A
authors.initials: SA
authors.lastname: Patil
authors.forename: Shivkumar S
authors.initials: SS
authors.lastname: Jalde
authors.forename: Basawaraj A
authors.initials: BA
authors.lastname: Koti
authors.forename: Nagesh A
authors.initials: NA
authors.lastname: Dhole
authors.forename: Rajesh N
authors.initials: RN
authors.lastname: Gacche
authors.forename: Amol
authors.initials: A
authors.lastname: Shirfule
mesh_terms: D000284:Administration, Oral; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D016588:Anticarcinogenic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000737:chemistry*; D045744:Cell Line, Tumor; D047188:Chalcones / Q000737:chemistry*; D060326:Chemistry Techniques, Synthetic; D004354:Drug Screening Assays, Antitumor; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
chemical_list: D000890:Anti-Infective Agents; D016588:Anticarcinogenic Agents; D000935:Antifungal Agents; D000975:Antioxidants; D002227:Carbazoles; D047188:Chalcones; D016166:Free Radical Scavengers; C041514:carbazole