By Alan C. Sartorelli (Eds.)
content material: improvement of [alpha]-(N)-heterocyclic carboxaldehyde thiosemicarbazones with medical power as antineoplastic brokers / Alan C. Sartorelli and Krishna C. Agrawal --
Adriamycin / David W. Henry --
Biochemical pharmacology of the anthracycline antibiotics / Nicholas R. Bachur --
power bioreductive alkylating brokers / Ai Jeng Lin, Lucille A. Cosby, and Alan C. Sartorelli --
A evaluation of experiences at the mechanism of motion of nitrosoureas / Glynn P. Wheeler.
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Extra info for Cancer Chemotherapy
B D a t a from r e f . 100. c Data from r e f . 84. ; ACS Symposium Series; American Chemical Society: Washington, DC, 1976. b 2. HENRY Adriamycin 29 a c t i v i t y i s r e t a i n e d a f t e r i n s e r t i o n of such a l a r g e and comp a r a t i v e l y nonpolar group. Carbonyl d e r i v a t i z a t i o n at C-13 a l s o causes a decrease i n potency i n animal t e s t s but the e f f e c t i s l e s s than with Na c y l a t i o n and the e f f i c a c y of the d e r i v a t i v e i s o c c a s i o n a l l y b e t t e r than the parent a n t i b i o t i c .
Compound 49 possessed a b i n d i n g constant about one-half that of adriamycin^but the apparent number of receptor s i t e s was e q u i v a l e n t to the a n t i b i o t i c . No b i o l o g i c a l data on these compounds have been published but i t i s s i g n i f i c a n t that such r e l a t i v e l y a c c e s s i b l e and simple analogs e x h i b i t DNA b i n d i n g c h a r a c t e r i s t i c s very s i m i l a r t o those of the much more complex parent a n t i b i o t i c s . ; ACS Symposium Series; American Chemical Society: Washington, DC, 1976.
Dall'acqu chroism experiments tha adriamycin are p e r p e n d i c u l a r to the DNA h e l i x a x i s (64). Waring demonstrated that i n c r e a s i n g c o n c e n t r a t i o n s of daunomycin e f f e c t r e v e r s a l of the s u p e r c o i l s of 0X174 closed c i r c u l a r DNA, a phenomenon considered h i g h l y d i a g n o s t i c f o r i n t e r c a l a t i o n (65). Pigram et a l . studied f i b e r s of DNA-daunomycin complex by X-ray d i f f r a c t i o n and concluded that the p a t t e r n s obtained were c o n s i s t e n t only w i t h i n t e r c a l a t i v e b i n d i n g (66).
Cancer Chemotherapy by Alan C. Sartorelli (Eds.)