Lexitropsin
Lexitropsins are members of a family of semi-synthetic DNA-binding ligands.{{cite journal |author1=Sondhi S.M. |author2=Praveen Reddy B.S. |author3=Lown J.W. |title= Lexitropsin conjugates: Action on DNA targets |journal= Current Medicinal Chemistry |volume=4 |pages=313–358 |year=1997|issue=5 |doi=10.2174/0929867304666220313122616 |s2cid=247445486 }} They are structural analogs of the natural antibiotics netropsin and distamycin. Antibiotics of this group can bind in the minor groove of DNA with different sequence-selectivity.{{cite journal |doi= 10.1021/bi00051a013 |last1=Goodsell |first1=D.S. |last2=Ng |first2=H.L. |last3=Kopka |first3=M.L. |last4=Lown |first4=J.W. |last5=Dickerson |first5=R.E. |title= Structure of a dicationic monoimidazole lexitropsin bound to DNA |journal= Biochemistry |volume= 34 |pages= 16654–61 |year= 1995 |pmid= 8527438 |issue= 51}}{{cite journal |last= Goodsell |first= D.S. |title= Sequence recognition of DNA by lexitropsins |journal= Curr Med Chem |volume= 8 |pages= 509–16 |year= 2001 |pmid= 11281838 |issue= 5 |doi=10.2174/0929867003373319}} Lexitropsins form a complexes with DNA with stoichiometry 1:1 and 2:1. Based on the 2:1 complexes were obtained ligands with high sequence-selectivity.{{cite journal |last1=Kopka |first1=M.L. |last2=Goodsell |first2=D.S. |last3=Han |first3=G. Won |last4=Chiu |first4=Th.K. |last5=Lown |first5=J.W. |last6=Dickerson |first6=R.E. |title= Defining GC-specificity in the minor groove: side-by-side binding of the di-imidazole lexitropsin to C-A-T-G-G-C-C-A-T-G |journal= Structure |volume= 5 |pages= 1033–1046 |year= 1997 |issue=8 |doi=10.1016/s0969-2126(97)00255-4|pmid=9309219 |doi-access=free }} This property is due to their selectivity towards AT-rich regions.{{Cite journal |last=Drozdowska |first=Danuta |last2=Bruzgo |first2=Irena |last3=Midura-Nowaczek |first3=Krystyna |date=2010-10-01 |title=Carbocyclic potential DNA minor groove binders and their biological evaluation |url=https://www.tandfonline.com/doi/full/10.3109/14756360903389872 |journal=Journal of Enzyme Inhibition and Medicinal Chemistry |volume=25 |issue=5 |pages=629–634 |doi=10.3109/14756360903389872 |issn=1475-6366 |pmid=20429779|url-access=subscription }}
File:Carbocyclilc lexitropsin analogues.png
Recently, carbocyclic derivatives based on pentamidine were shown to exhibit in vivo antiproliferative effects on human breast cancer cells, possibly because of their ability to inhibit topoisomerase activity.{{Cite journal |last=Arciszewska |first=Karolina |last2=Pućkowska |first2=Anna |last3=Wróbel |first3=Agnieszka |last4=Drozdowska |first4=Danuta |date=2018-12-06 |title=Carbocyclic Analogues of Distamycin and Netropsin |url=http://www.eurekaselect.com/166096/article |journal=Mini-Reviews in Medicinal Chemistry |language=en |volume=19 |issue=2 |pages=98–113 |doi=10.2174/1389557518666181009143203|url-access=subscription }}{{Cite journal |last=Drozdowska |first=Danuta |last2=Rusak |first2=Malgorzata |last3=Miltyk |first3=Wojciech |last4=Midura-Nowaczek |first4=Krystyna |date=2009 |title=Synthesis and Biological Evaluation of Distamycin Analogues – New Potential Anticancer Agents |url=https://onlinelibrary.wiley.com/doi/10.1002/ardp.200800122 |journal=Archiv der Pharmazie |language=en |volume=342 |issue=2 |pages=87–93 |doi=10.1002/ardp.200800122 |issn=1521-4184|url-access=subscription }}