- Synthesis of new praziquantel analogues: Potential candidates for the treatment of schistosomiasis
[作者：Sadhu, PS; Kumar, SN; Chandrasekharam, M; Pica-Mattoccia, L; Cioli, D; Rao, VJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1103-1106 , 文章类型： Article，,卷期：2012年22-2]
- An efficient synthesis of antischistosomal drug praziquantel and analogues was achieved and the synthetic route designed was to afford structurally diverse analogues for better structure-activity relationship understandi...
- Synthesis and anti-HCV activity evaluation of anilinoquinoline derivatives
[作者：Peng, HK; Lin, CK; Yang, SY; Tseng, CK; Tzeng, CC; Lee, JC; Yang, SC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1107-1110 , 文章类型： Article，,卷期：2012年22-2]
- Hepatitis C virus (HCV) infection is a main cause of chronic liver disease, leading to liver cirrhosis and hepatocellular carcinoma (HCC). The objective of our research was to develop effective agents against viral repli...
- Discovery of potent, selective and orally bioavailable triaryl-sulfonamide based PTP1B inhibitors
[作者：Patel, D; Jain, M; Shah, SR; Bahekar, R; Jadav, P; Joharapurkar, A; Dhanesha, N; Shaikh, M; Sairam, KVVM; Kapadnis, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1111-1117 , 文章类型： Article，,卷期：2012年22-2]
- A novel series of pTyr mimetics containing triaryl-sulfonamide derivatives (5a-r) are reported as potent and selective PTP1B inhibitors. Some of the test compounds (50 and 5p) showed excellent selectivity towards PTP1B o...
- Synthesis and biological evaluation of 7-O-modified oroxylin A derivatives
[作者：Fu, W; Wang, JB; Yu, LQ; Zhao, L; Lu, N; You, QD; Guo, QL; Li, ZY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1118-1121 , 文章类型： Article，,卷期：2012年22-2]
- Oroxylin A (5,7-dihydroxy-6-methoxyflavone) is a naturally occurring monoflavonoid isolated from the root of Scutellaria baicalensis Georgi, and exhibits potent anticancer activities in vitro and in vivo. In this study, ...
- Symmetric dimers of ent-kaurane diterpenoids with cytotoxic activity from Croton tonkinensis
[作者：Thuong, PT; Thi, HMP; Thi, VTL; Dao, TT; Dang, TT; Nguyen, QT; Oh, WK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1122-1124 , 文章类型： Article，,卷期：2012年22-2]
- Breast cancer is the most common malignant tumor in women these days accounting for approximately 24% of all cancer. During our screening program searching for cytotoxic materials from natural products, two new symmetric...
- Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation
[作者：Brullo, C; Rocca, M; Fossa, P; Cichero, E; Barocelli, E; Ballabeni, V; Flammini, L; Giorgio, C; Saccani, F; Domenichini, G; Bruno, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1125-1129 , 文章类型： Article，,卷期：2012年22-2]
- In pursuing our research on some 2,4-diamino-benzopyranopyrimidines and 2-amino-5,6-dihydrobenzo[h]quinazolines, previously reported as antiplatelet and analgesic/anti-inflammatory agents respectively, we designed and sy...
- Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design
[作者：Hamada, Y; Tagad, HD; Nishimura, Y; Ishiura, S; Kiso, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1130-1135 , 文章类型： Article，,卷期：2012年22-2]
- Previously reported pentapeptidic BACE1 inhibitors, designed using a substrate-based approach, were used as lead compounds for the further design of non-peptidic BACE1 inhibitors. Although these peptidic and non-peptidic...
- Design and synthesis of novel macrocyclic 2-amino-6-arylpyrimidine Hsp90 inhibitors
[作者：Suda, A; Koyano, H; Hayase, T; Hada, K; Kawasaki, K; Komiyama, S; Hasegawa, K; Fukami, TA; Sato, S; Miura, T; Ono, N; Yamazaki, T; Saitoh, R; Shimma, N; Shiratori, Y; Tsukuda, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1136-1141 , 文章类型： Article，,卷期：2012年22-2]
- Macrocyclic compounds bearing a 2-amino-6-arylpyrimidine moiety were identified as potent heat shock protein 90 (Hsp90) inhibitors by modification of 2-amino-6-aryltriazine derivative (CH5015765). We employed a macrocycl...
- Promoting the formation of tetramolecular G-quadruplexes under freezing condition
[作者：Zhai, QQ; Deng, MG; Xu, L; Zhang, XL; Zhou, X,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1142-1145 , 文章类型： Article，,卷期：2012年22-2]
- In the study, we demonstrated that freezing was able to facilitate the short DNA strand T(4)G(4) to self-assemble into a tetramolecular G-quadruplex with a low DNA concentration in the absence of any ligand, providing a ...
- Cu-mediated N-arylation of 1,2,3-triazin-4-ones: Synthesis of fused triazinone derivatives as potential inhibitors of chorismate mutase
[作者：Kumar, KS; Adepu, R; Sandra, S; Rambabu, D; Krishna, GR; Reddy, CM; Misra, P; Pal, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1146-1150 , 文章类型： Article，,卷期：2012年22-2]
- A rapid and direct access to N-aryl substituted fused triazinone derivatives has been accomplished via N-arylation of 1,2,3-triazin-4-one ring involving a Cu-mediated coupling between triazinone derivatives and aryl boro...
- High-affinity fluorescent ligands for the 5-HT3 receptor
[作者：Simonin, J; Vernekar, SKV; Thompson, AJ; Hothersall, JD; Connolly, CN; Lummis, SCR; Lochner, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1151-1155 , 文章类型： Article，,卷期：2012年22-2]
- The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high aff...
- Synthesis of novel histamine H4 receptor antagonists
[作者：Lane, CAL; Hay, D; Mowbray, CE; Paradowski, M; Selby, MD; Swain, NA; Williams, DH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1156-1159 , 文章类型： Article，,卷期：2012年22-2]
- This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound 20 was found to be a potent and selective histamine...
- Novel substituted pyrimidines as HCV replication (replicase) inhibitors
[作者：Kwong, CD; Clark, JL; Fowler, AT; Geng, F; Kezar, HS; Roychowdhury, A; Reynolds, RC; Maddry, JA; Ananthan, S; Secrist, JA; Shih, NY; Piwinski, JJ; Li, C; Feld, B; Huang, HC; Tong, X; Njoroge, G; Arasappan, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1160-1164 , 文章类型： Article，,卷期：2012年22-2]
- Compound I was identified as a HCV replication inhibitor from screening/early SAR triage. Potency improvement was achieved via modulation of substituent on the 5-azo linkage. Due to potential toxicological concern, the 5...
- Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties
[作者：Ren, L; Laird, ER; Buckmelter, AJ; Dinkel, V; Gloor, SL; Grina, J; Newhouse, B; Rasor, K; Hastings, G; Gradl, SN; Rudolph, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1165-1168 , 文章类型： Article，,卷期：2012年22-2]
- Herein we describe a novel series of ATP competitive B-Rat inhibitors based on the pyrazolo[1,5-a]pyrimidine scaffold. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. Optimization...
- Multiparameter exploration of piperazine derivatives as delta-opioid receptor agonists for CNS indications
[作者：McCauley, JP; Dantzman, CL; King, MM; Ernst, GE; Wang, X; Brush, K; Palmer, WE; Frietze, W; Andisik, DW; Hoesch, V; Doring, K; Hulsizer, J; Bui, KH; Liu, J; Hudzik, TJ; Wesolowski, SS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：1169-1173 , 文章类型： Article，,卷期：2012年22-2]
- A novel series of piperazine derivatives exhibits sub-nanomolar binding and enhanced subtype selectivity as delta-opioid agonists. The synthesis and SAR are described as well as the application of computational models to...
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