10.1186/1472-6769-12-5BMC Chemical Biology12

Anilkumar, N.C.

Basappa

Li, F.

Manu, K.A.

Nanjundaswamy, S.

Prasanna, D.S.

Rangappa, K.S.

Sadashiva, M.P.

Sengottuvelan, M.

Sethi, G.

Sugahara, K.

PubMed

Basappa Basappa

sadashiva M P

Nanjundaswamy S

Gautam Sethi

Manoj Aryan

Feng Li

Sengottuvelan Murugan

prasanna D S

kazuyuki Sugahara

Rangappa S K

Springer - Publisher Connector

Anti-cancer activity of novel dibenzo[b,f]azepine tethered isoxazoline derivatives

Dibenzoazepine (DB) derivatives are important and valuable compounds in medicinal chemistry. The synthesis and chemotherapeutic properties of naturally occurring DBs and different heterocyclic moiety tethered DBs are reported. Herein, we report the DB-fused hybrid structure that containing isoxazolines (DBIs) and their anti-cancer activity, which could throw light on the structural and functional features of new molecules

Maralinganadoddi Panchegowda Sadashiva, .

Basappa, .

Shivananju NanjundaSwamy, .

Feng Li, .

Kanjoormana Aryan Manu, .

Murugan Sengottuvelan, .

Doddakunche Shivaramu Prasanna, .

Nirvanappa Chikkagundagal Anilkumar, .

Gautam Sethi, .

Kazuyuki Sugahara, .

Kanchugarakoppal Subbegowda Rangappa, .

ePrints@Bangalore University

Background

Dibenzoazepine (DB) derivatives are important and valuable compounds in medicinal chemistry. The synthesis and chemotherapeutic properties of naturally occurring DBs and different heterocyclic moiety tethered DBs are reported. Herein, we report the DB-fused hybrid structure that containing isoxazolines (DBIs) and their anti-cancer activity, which could throw light on the structural and functional features of new molecules.



Results and Conclusion

The synthesis and characterization of novel ring DB tethered isoxazoline derivatives (DBIs) were carried out. After the detailed structural characterization using 2D-NMR experiments, the compounds were identified as 5-substituted isoxazolines. The effect of newly synthesized DBIs against the invasion of murine osteosarcoma (LM8G7) cells was studied. Among the tested molecules, compound 4g (5-[−3-(4-chlorophenyl)-4,5-dihydroisoxazol-5-yl-methyl]-5 H- dibenzo[b,f]azepine), was found to inhibit the invasion of LM8G7 cells strongly, when compared to other structurally related compounds. Cumulatively, the compound 4g inhibited the invasion MDA-MB-231 cells completely at 10 μM. In addition to anti-invasion property the compound 4g also inhibited the migration of LM8G7 and human ovarian cancer cells (OVSAHO) dose-dependently. Compound 4g inhibited the proliferation of LM8G7, OVSAHO, human breast cancer cells (MCF-7) and human melphalan-resistant multiple myeloma (RPMI8226-LR5) cells that are comparable to cisplatin and suramin

Sadashiva, M. P.

Nanjunda Swamy, S.

Li, Feng

Manu, Kanjoormana Aryan

Sengottuvelan, Murugan

Prasanna, D. S.

Anilkumar, N. C.

Sethi, Gautam

Sugahara, Kazuyuki

Rangappa, K. S.

University of Mysore - Digital Repository of Research, Innovation and Scholarship (ePrints@UoM)

Anti-Cancer activity of Novel Dibenzo[B,f]Azepine Tethered Isoxazoline derivatives

Background: Dibenzoazepine (DB) derivatives are important and valuable compounds in medicinal chemistry. The synthesis and chemotherapeutic properties of naturally occurring DBs and different heterocyclic moiety tethered DBs are reported. Herein, we report the DB-fused hybrid structure that containing isoxazolines (DBIs) and their anti-cancer activity, which could throw light on the structural and functional features of new molecules. Results and Conclusion. The synthesis and characterization of novel ring DB tethered isoxazoline derivatives (DBIs) were carried out. After the detailed structural characterization using 2D-NMR experiments, the compounds were identified as 5-substituted isoxazolines. The effect of newly synthesized DBIs against the invasion of murine osteosarcoma (LM8G7) cells was studied. Among the tested molecules, compound 4g (5--3-(4-chlorophenyl)-4,5-dihydroisoxazol-5-yl-methyl- 5 H-dibenzob,fazepine), was found to inhibit the invasion of LM8G7 cells strongly, when compared to other structurally related compounds. Cumulatively, the compound 4g inhibited the invasion MDA-MB-231 cells completely at 10 Î¼M. In addition to anti-invasion property the compound 4g also inhibited the migration of LM8G7 and human ovarian cancer cells (OVSAHO) dose-dependently. Compound 4g inhibited the proliferation of LM8G7, OVSAHO, human breast cancer cells (MCF-7) and human melphalan-resistant multiple myeloma (RPMI8226-LR5) cells that are comparable to cisplatin and suramin. Â© 2012 Sadashiva et al.; licensee BioMed Central Ltd

Anti-cancer activity of novel dibenzob,fazepine tethered isoxazoline derivatives

Abstract
          
            Background
            Dibenzoazepine (DB) derivatives are important and valuable compounds in medicinal chemistry. The synthesis and chemotherapeutic properties of naturally occurring DBs and different heterocyclic moiety tethered DBs are reported. Herein, we report the DB-fused hybrid structure that containing isoxazolines (DBIs) and their anti-cancer activity, which could throw light on the structural and functional features of new molecules.
          
          
            Results and Conclusion
            The synthesis and characterization of novel ring DB tethered isoxazoline derivatives (DBIs) were carried out. After the detailed structural characterization using 2D-NMR experiments, the compounds were identified as 5-substituted isoxazolines. The effect of newly synthesized DBIs against the invasion of murine osteosarcoma (LM8G7) cells was studied. Among the tested molecules, compound 4g (5-[−3-(4-chlorophenyl)-4,5-dihydroisoxazol-5-yl-methyl]-5 H- dibenzo[b,f]azepine), was found to inhibit the invasion of LM8G7 cells strongly, when compared to other structurally related compounds. Cumulatively, the compound 4g inhibited the invasion MDA-MB-231 cells completely at 10 μM. In addition to anti-invasion property the compound 4g also inhibited the migration of LM8G7 and human ovarian cancer cells (OVSAHO) dose-dependently. Compound 4g inhibited the proliferation of LM8G7, OVSAHO, human breast cancer cells (MCF-7) and human melphalan-resistant multiple myeloma (RPMI8226-LR5) cells that are comparable to cisplatin and suramin.
          </jats:sec

Maralinganadoddi Panchegowda Sadashiva

null Basappa

Shivananju NanjundaSwamy

Kanjoormana Aryan Manu

Murugan Sengottuvelan

Doddakunche Shivaramu Prasanna

Nirvanappa Chikkagundagal Anilkumar

Kazuyuki Sugahara

Kanchugarakoppal Subbegowda Rangappa

Crossref

BMC Chemical Biology

3rd edition.

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Anti-cancer activity of novel dibenzo[b,f]azepine tethered isoxazoline derivatives

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