PubMed ID Title Abstract Journal Cited Gene Actors (Entries are '|' delimited) Cited Chemical Actors (Entries are '|' delimited) Cited Disease Actors (Entries are '|' delimited) Marked-up HTML of abstract with tagged links back to CTD for all actors and terms Document Relevancy Score Marked-up HTML of relevant sentences/phrases extracted with tagged links back to CTD for all actors and terms (sentences/phrases are '|' delimited) Cited Action Terms (Entries are '|' delimited) Cited Interactions (Entries are '|' delimited) 17368022 Analogs of the marine alkaloid makaluvamines: synthesis, topoisomerase II inhibition, and anticancer activity. Twelve analogs of makaluvamines have been synthesized. These compounds were evaluated for their ability to inhibit the enzyme topoisomerase II. Five compounds were shown to inhibit topoisomerase catalytic activity comparable to two known topoisomerase II targeting control drugs, etoposide and m-AMSA. Their cytotoxicity against human colon cancer cell line HCT-116 and human breast cancer cell lines MCF-7 and MDA-MB-468 has been evaluated. Four makaluvamine analogs exhibited better IC(50) values against HCT-116 as compared to control drug etoposide. One analog exhibited better IC(50) value against HCT-116 as compared to m-AMSA. All 12 of the makaluvamine analogs exhibited better IC(50) values against MCF-7 and MDA-MB-468 as compared to etoposide as well as m-AMSA. Bioorg Med Chem Lett TOP2A AMSACRINE|ETOPOSIDE COLONIC NEOPLASMS|BREAST NEOPLASMS Twelve analogs of makaluvamines have been synthesized. These compounds were evaluated for their ability to inhibit the enzyme TOPOISOMERASE II. Five compounds were shown to inhibit TOPOISOMERASE catalytic activity comparable to two known TOPOISOMERASE II targeting control drugs, ETOPOSIDE and M-AMSA. Their cytotoxicity against human COLON CANCER cell line HCT-116 and human BREAST CANCER cell lines MCF-7 and MDA-MB-468 has been evaluated. Four makaluvamine analogs exhibited better IC(50) values against HCT-116 as compared to control drug ETOPOSIDE. One analog exhibited better IC(50) value against HCT-116 as compared to M-AMSA. All 12 of the makaluvamine analogs exhibited better IC(50) values against MCF-7 and MDA-MB-468 as compared to ETOPOSIDE as well as M-AMSA. 0.5 Five compounds were shown to inhibit TOPOISOMERASE catalytic activity comparable to two known TOPOISOMERASE II targeting control drugs, ETOPOSIDE and M-AMSA.|Four makaluvamine analogs exhibited better IC(50) values against HCT-116 as compared to control drug ETOPOSIDE. |All 12 of the makaluvamine analogs exhibited better IC(50) values against MCF-7 and MDA-MB-468 as compared to ETOPOSIDE as well as M-AMSA. decreases activity Etoposide results in decreased activity of TOP2A protein|Amsacrine results in decreased activity of TOP2A protein