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Structural Modifications of Bryostatin 2

Structural Modifications of Bryostatin 2

G R Pettit, D Sengupta, P M Blumberg, N E Lewin, J M Schmidt, A S Kraft

Anticancer Drug Des. 1992 Apr;7(2):101-14.

PMID: 1575884

Abstract:

Continuation of a structure/activity relationship study of the bryostatins was focused on bryostatin 2. Stepwise catalytic hydrogenation of bryostatin 2 gave the following results. Reduction of the side-chain diene system to saturated ester 2a (P388 cell line ED50 8.5 x 10(-3) micrograms/ml) did not significantly affect the murine P388 cell line inhibition by bryostatin 2. Further hydrogenation to hexahydro derivative 2b gave a reduced P388 ED50 of 5.1 x 10(-2) micrograms/ml. Conversion to the octahydrobryostatin 2c caused a further reduction of P388 cell line activity to ED50 2.9 x 10(-1) micrograms/ml. Other structural modifications of bryostatin 2 in respect to esterification at the C-7 position significantly affected the P388 lymphocytic leukemia cell line response. Each of the bryostatin 2 derivatives was also evaluated with respect to protein kinase C binding.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP87745286	Bryostatin 2		87745-28-6	Price

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