title: Synthesis and biological evaluation of novel quinazoline-sulfonamides as anti-cancer agents.
abstract: A robust economic approach to N-(quinazoline-4-yl)sulfonamides was developed and synthesized different aryl, hetero aryl, alkyl and cyclopropyl sulfonamides in excellent yields. All the compounds were evaluated for cytotoxic affinity to SKOV3, DU145, THP1, U937, and COLO205 cell lines. Interesting to find that the bulkiness of substituent at C-2 position of quinazoline forces the molecule to flip around in order to bind in the active site, when compared to the binding preference of previously known quinazoline compounds. Among the 21 compounds synthesized 2b, 2d, 2e, 2h, 2i, 3c, 3d, 3f, 3g and 3h found to be active on all the cell lines tested with IC50values <10µg/mL. Performed docking simulations to understand the binding preference of various C-2 substituted quinazoline sulfonamides.
authors.affiliation: Medicinal Chemistry Division, GVK Biosciences Pvt. Ltd, Plot 28A, IDA Nacharam, Hyderabad, India; JNTUH-College of Engineering, Nachupally, Karimnagar, India.
authors.forename: Suresh
authors.initials: S
authors.lastname: Poudapally
authors.affiliation: Medicinal Chemistry Division, GVK Biosciences Pvt. Ltd, Plot 28A, IDA Nacharam, Hyderabad, India.
authors.forename: Shankar
authors.initials: S
authors.lastname: Battu
authors.affiliation: Biology Division, Indian Institute of Chemical Technology, Hyderabad 500 007, AP, India.
authors.forename: Loka Reddy
authors.initials: LR
authors.lastname: Velatooru
authors.affiliation: Biology Division, Indian Institute of Chemical Technology, Hyderabad 500 007, AP, India.
authors.forename: Murali Satyanarayana
authors.initials: MS
authors.lastname: Bethu
authors.affiliation: Biology Division, Indian Institute of Chemical Technology, Hyderabad 500 007, AP, India.
authors.forename: Venkateswara Rao
authors.initials: VR
authors.lastname: Janapala
authors.affiliation: Medicinal Chemistry Division, GVK Biosciences Pvt. Ltd, Plot 28A, IDA Nacharam, Hyderabad, India.
authors.forename: Somesh
authors.initials: S
authors.lastname: Sharma
authors.affiliation: Department of Chemistry, School of Natural Sciences, Shiv Nadar University, UP 201314, India.
authors.forename: Subhabrata
authors.initials: S
authors.lastname: Sen
authors.affiliation: Medicinal Chemistry Division, GVK Biosciences Pvt. Ltd, Plot 28A, IDA Nacharam, Hyderabad, India.
authors.forename: Narender
authors.initials: N
authors.lastname: Pottabathini
authors.affiliation: Medicinal Chemistry Division, GVK Biosciences Pvt. Ltd, Plot 28A, IDA Nacharam, Hyderabad, India. Electronic address: vijayabhaskara.iska@gvkbio.com.
authors.forename: Vijaya Bhaskara Reddy
authors.initials: VBR
authors.lastname: Iska
authors.affiliation: JNTUH-College of Engineering, Nachupally, Karimnagar, India. Electronic address: vidyaorg@yahoo.com.
authors.forename: Vidya
authors.initials: V
authors.lastname: Katangoor
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; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D062105:Molecular Docking Simulation; D009369:Neoplasms / Q000188:drug therapy; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines; D013449:Sulfonamides