186805-48-1Relevant academic research and scientific papers
Synthesis and Biological Evaluation of Amidinourea and Triazine Congeners as Inhibitors of MDA-MB-231 Human Breast Cancer Cell Proliferation
Bass, Rosemary,Jenkinson, Sarah,Wright, Jennifer,Smulders-Srinivasan, Tora,Marshall, Jamie C.,Castagnolo, Daniele
, p. 288 - 291 (2017)
A series of novel amidinourea derivatives was synthesized, and the compounds were evaluated as inhibitors of MDA-MB-231 human breast cancer cell proliferation. In addition, a second series of triazine derivatives designed as rigid congeners of the amidinoureas was synthesized, and the compounds were evaluated for their antiproliferative activity. Among the two series, amidinourea 3 d (N-[N-[8-[[N-(morpholine-4-carbonyl)carbamimidoyl]amino]octyl]carbamimidoyl]morpholine-4-carboxamide) emerged as a potent anticancer hit compound with an IC50value of 0.76 μm, similar to that of tamoxifen.
Heterocyclic compounds as well as preparation method and application thereof
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Paragraph 0221; 0222; 0223; 0309; 0310, (2018/07/30)
The invention belongs to the field of medicines and particularly relates to heterocyclic compounds with the structural characteristics shown in formula (I) or pharmaceutically acceptable salts, a preparation method and an application of the heterocyclic compounds as a nucleotide oxidative damage repairase MTH1 inhibitor. Pharmacological experiment results indicate that the compounds have significant inhabitation effects on the activity of MTH1 and can be used for preventing and treating clinical diseases related to MTH1.
Screening for novel antimicrobials from encoded combinatorial libraries by using a two-dimensional agar format
Silen, Joy L.,Lu, Amy T.,Solas, Dennis W.,Gore, Medini A.,Maclean, Derek,Shah, Nikil H.,Coffin, Jill M.,Bhinderwala, Naseema S.,Wang, Yongwen,Tsutsui, Ken T.,Look, Gary C.,Campbell, David A.,Hale, Ron L.,Navre, Marc,Deluca-Flaherty, Camille R.
, p. 1447 - 1453 (2007/10/03)
A sensitive lawn-based format has been developed to screen bead-tethered combinatorial chemical libraries for antimicrobial activity. This method has been validated with beads linked to penicillin V via a photocleavable chemical linker in several analyses including a spike-and-recover experiment. The lawn-based screen sensitivity was modified to detect antibacterial compounds of modest potency, and a demonstration experiment with a naive combinatorial library of over 46,000 individual triazines was evaluated for antibacterial activity. Numerous hits were identified, and both active and inactive compounds were resynthesized and confirmed in traditional broth assays. This demonstration experiment suggests that novel antimicrobial compounds can be easily identified from very large combinatorial libraries of small, nonpeptidic compounds.
