title: Synthesis of oxadiazole-morpholine derivatives and manifestation of the repressed CD31 Microvessel Density (MVD) as tumoral angiogenic parameters in Dalton's Lymphoma.
abstract: A series of oxadiazole derivatives possessing morpholine 6a-l were synthesized by nucleophilic substitution reaction of key intermediates [1,3,4]-oxadiazole-2-thiol derivatives 5a-l with 4-(2-chloroethyl) morpholine. Compounds 6a-l were evaluated for their in vitro and in vivo antitumor potential in Dalton's Lymphoma Ascites (DLA) tumor cells. Among 6a-l series, compound 6a with concentration ∼8.5μM have shown extensive cytotoxicity in vitro and 85% reduction in tumor volume in vivo, attributing an excellent anti-proliferative capability towards the cancer cells. Compound 6a has extensively inhibited the Microvessel Density (MVD) or tumoral neovasculature which was evident from the CD31 immuno staining and peritoneal H&E staining. The major reason for the antiproliferative activity of compound 6a was due to the repression of tumor vasculature.
authors.affiliation: Department of Chemistry, Yuvaraja's college, University of Mysore, Mysore 570005, Karnataka, India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Al-Ghorbani
authors.affiliation: Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (Autonomous), Kuvempu University, Shimoga 577203, Karnataka, India.
authors.forename: V
authors.initials: V
authors.lastname: Vigneshwaran
authors.affiliation: Department of Chemistry, Yuvaraja's college, University of Mysore, Mysore 570005, Karnataka, India; PG Department of Chemistry, St. Philomena's College, Mysore 570015, India.
authors.forename: V Lakshmi
authors.initials: VL
authors.lastname: Ranganatha
authors.affiliation: Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (Autonomous), Kuvempu University, Shimoga 577203, Karnataka, India.
authors.forename: B T
authors.initials: BT
authors.lastname: Prabhakar
authors.affiliation: Department of Chemistry, Yuvaraja's college, University of Mysore, Mysore 570005, Karnataka, India. Electronic address: shaukathara@yahoo.co.in.
authors.forename: Shaukath Ara
authors.initials: SA
authors.lastname: Khanum
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D001201:Ascites / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D008223:Lymphoma / Q000188:drug therapy* / Q000473:pathology; D051379:Mice; D055806:Microvessels / Q000187:drug effects* / Q000473:pathology; D009025:Morpholines / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D009389:Neovascularization, Pathologic / Q000188:drug therapy* / Q000473:pathology; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D009025:Morpholines; D010069:Oxadiazoles; C037574:morpholine
keywords: Angiogenesis; CD31; Dalton’s Lymphoma; Microvessel Density (MVD); Oxadiazole–morpholine