ライフサイエンスコーパス: dictyostatin

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1 shown to retain the low nanomolar potency of dictyostatin.

2 esis that produced more than 30 mg of 6- epi-dictyostatin.

3 Four analogs (6-epi-dictyostatin, 7-epi-dictyostatin, 16-normethyldictyostatin, and 15Z,16-norme

4 Four analogs (6-epi-dictyostatin, 7-epi-dictyostatin, 16-normethyldictyostat

5 Dictyostatin also induces assembly of purified tubulin m

6 y in paclitaxel-resistant cell lines, making dictyostatin an attractive candidate for development as

7 In this study, we examined a series of dictyostatin analogs to probe biological and biochemical

8 chosen as potentially potent yet accessible dictyostatin analogues, and three new syntheses were dev

9 g site than paclitaxel, indicated that 6-epi-dictyostatin and 7-epi-dictyostatin displaced [(14)C]epo

10 tently than any other compound examined, and dictyostatin and discodermolide had equivalent activity

11 Detailed comparison of the abilities of dictyostatin and discodermolide to induce tubulin assemb

12 n, establish a validated linker strategy for dictyostatin, and set the stage for the synthesis and st

13 The dictyostatins are a promising class of potential anti-ca

14 or linker attachment, and its application to dictyostatin, are described.

15 The naturally occurring compound (-)-dictyostatin binds to MTs, causes cell cycle arrest in G

16 set the stage for the synthesis and study of dictyostatin conjugates.

17 Dictyostatin (DCT, 1) is a complex, flexible polyketide

18 The antiproliferative activity of dictyostatin did not differ greatly from that of paclita

19 indicated that 6-epi-dictyostatin and 7-epi-dictyostatin displaced [(14)C]epothilone B with K(i) val

20 paclitaxel, epothilones A/B, discodermolide, dictyostatin, eleutherobin, the steroid derivative 17bet

21 d on the naturally occurring antitumor agent dictyostatin have recently identified several highly act

22 The work provided several new analogues of dictyostatin, including a truncated macrolactone and a C

23 Dictyostatin inhibited the binding of radiolabeled disco

24 (-)-Dictyostatin is a sponge-derived, 22-member macrolactone

25 of a precursor to the C11-C23 segment of (-)-dictyostatin is described.

26 h the idea that the macrocyclic structure of dictyostatin represents the template for the bioactive c

27 h were 400- and 50-fold less active than (-)-dictyostatin, respectively.

28 Like discodermolide, dictyostatin retained antiproliferative activity against

29 paclitaxel, and nearly as vigorously as does dictyostatin's close structural congener, (+)-discodermo

30 lts portray a diversity of conformations for dictyostatin that illustrates the molecule's flexibility

31 and cellular toxicity to identify regions of dictyostatin that were essential for biological activity

32 , these results shed light on the binding of dictyostatin to beta-tubulin, establish a validated link

33 We used synthetic (-)-dictyostatin to study its biochemical and cytological ac

34 From these compounds, 6- epi-dictyostatin was selected for scaleup preparation and ev

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