SYNTHESIS OF (-) ¿ PYRENOPHOROL, ANTICANCER EVALUATION OF HETEROCYCLES - EDUKONDALU, PERUGU
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The total synthesis of (-)-pyrenophorol with high enantio selectivity has been accomplished in which the stereocenters were established by Jacobsen's hydrolytic kinetic resolution and Sharpless asymmetric dihydroxylation and cyclization was achieved by intermolecular Mitsunobu cyclization. The compound 90b with electron donating 3,4,5-trimethoxy group on the phenyl ring, showed excellent anticancer activity (MCF-7 = 0.018±0.0039 miM, A549 = 0.011±0.0019 miM, Colo-205 = 0.12±0.029 miM and A2780 = 0.17±0.023 miM) than etoposide. The compound 117i having electron-rich on the phenyl moiety showed…mehr

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Produktbeschreibung
The total synthesis of (-)-pyrenophorol with high enantio selectivity has been accomplished in which the stereocenters were established by Jacobsen's hydrolytic kinetic resolution and Sharpless asymmetric dihydroxylation and cyclization was achieved by intermolecular Mitsunobu cyclization. The compound 90b with electron donating 3,4,5-trimethoxy group on the phenyl ring, showed excellent anticancer activity (MCF-7 = 0.018±0.0039 miM, A549 = 0.011±0.0019 miM, Colo-205 = 0.12±0.029 miM and A2780 = 0.17±0.023 miM) than etoposide. The compound 117i having electron-rich on the phenyl moiety showed greater anticancer property on all cell lines (PC3=0.11±0.068 miM; A549=0.18±0.063 miM; MCF-7= 0.52±0.074 miM and DU-145=0.17±0.082 miM).
Autorenporträt
Dr. Perugu Edukondalu awarded his Ph.D Degree under the supervision of Prof. R. Ramesh Raju, Department of Chemistry, Acharya Nagarjuna University, Nagarjuna Nagar, Guntur, Andhra Pradesh, India. He Published his articles in national and international journals followed by in seminars and conferences.