Synthesis and evaluation of antimitotic activity of alkylated 2-amino-1,3,4-oxadiazole derivatives.
Series of N-alkylated-2-amino-1,3,4-oxadiazoles (2) were synthesized via alkylation of 2-amino-1,3,4-oxadiazoles (1) under phase transfer condition. This paper also describes the study of antimitotic activity of these molecules by onion root tip method.
Biological assay and antimitotic activity of synthetic derivatives of podophyllotoxin.
Of 17 podophyllotoxin [518-28-5] derivs. and podophyllins, the I²-apopicropodophyllin [477-52-1] (I) derivs. I epoxide [104759-36-6] I cyclic amide [104720-03-8], and I allylic amine [104759-37-7] were the most active antimitotic agents, whereas I²-apopicropodophyllyl dialdehyde [104701-04-4] and picropodophyllin [477-47-4] were the least active in the onion-root tip test of Sharma (1965) . Thus, functionalization of hydroarom. ring B of I with NH2 or an epoxide ring enhanced the antimitotic activity. Also, increase of the size of hydroarom. ring B as in podophyllohomotoxone [104701-02-2] and oxygenation of the ring B as in I²-apopicropodophyllone [101766-82-9] decreased the activity. Among the 3 parent podophyllins activity decreased in the order: I > podophyllotoxin >> picropodophyllin. [on SciFinder(R)]
Fungal Biotransformations in Pharmaceutical Sciences
The regio- and stereoselective conversion of complex substrates represents one of the major advantage of microbial biotransformation. This chapter covers the biocatalytic capacities of fungi to derivatize bioactive small molecules, both from natural sources and from synthetic compounds. We focus particularly on sterol and taxane biotransformation. We also present examples at the interface of biotransformation and pathway engineering using recombinant organisms, with an emphasis on the production of lovastatin derivatives. Finally, we highlight selected studies on fungal xenometabolism which serves as a model to study the breakdown of drugs in mammals.