Netropsin analogues

For review of distamycin and netropsin analogues Bailly, C. and Chaires, J. B. (1998) Sequence-specific DNA minor groove binders. Design and synthesis of netropsin and distamycin analogues. Bioconjugate Chem. 9,513-538. 

In the search for simpler analogues of netropsine and distamycin A, which are DNA minor groove binding antibiotics, pyrazoles (316) and (317) have been synthesized <89JOC428). The x-ray structure of (316) was reported. 

A 6(5-cationic thiazole analogue (281) of the minor groove binder netropsin has been shown to interact with the minor groove of AT rich regions despite the availability of thiazole... 

A number of synthetic analogues of distamycin and netropsin have been found to have excellent antitumor activity. For example, FCE 24517 (41), which is a nitrogen mustard-distamycin hybrid, is in clinical trials . The distamycin derivative (42) has increased water solubihty and enhanced cellular uptake <95H(4l)337>, and (43) is one of several related antitumor compounds with... 

---