Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors

• Chao Che,
• Song Li,
• Bo Yang,
• Shengchang Xin,
• Zhixiong Yu,
• Taofeng Shao,
• Chuanye Tao,
• Shuo Lin and
• Zhen Yang

Beilstein J. Org. Chem. 2012, 8, 841–849, doi:10.3762/bjoc.8.94

• secondary alkylamine due to the different conformational changes induced. This promising result prompted us to further investigate the structure–activity relationships (SAR) of Sant-75. Herein we describe our efforts in the development of synthetic methods for the construction of a library of Sant-75

Synthetic glycopeptides and glycoproteins with applications in biological research

• Ulrika Westerlind

Beilstein J. Org. Chem. 2012, 8, 804–818, doi:10.3762/bjoc.8.90

• ]. Synthetic glycoproteins An important task for chemists is to make homogenous glycoproteins and complex glycopeptides available for biological research. Studies of glycosylation effects on protein conformation, stability and structure–activity relationships (SAR) are a few examples of the applications of

Phytoalexins of the Pyrinae: Biphenyls and dibenzofurans

• Cornelia Chizzali and
• Ludger Beerhues

Beilstein J. Org. Chem. 2012, 8, 613–620, doi:10.3762/bjoc.8.68

• did [12], whereas the opposite tendency was observed for antifungal activity [26]. However, more biphenyls and dibenzofurans need to be tested for their antibacterial and antifungal potentials in order to allow for reliable conclusions concerning structure–activity relationships. The array of

Planar-bilayer activities of linear oligoester bolaamphiphiles

• Jonathan K. W. Chui,
• Thomas M. Fyles and
• Horace Luong

Beilstein J. Org. Chem. 2011, 7, 1562–1569, doi:10.3762/bjoc.7.184

• -molecule structure–activity relationships for compounds 1–8. Grids are given in the following sequence in each case: Square-top (green); flicker (yellow); multiple-opening (blue); spike (red); erratic (purple). Yellow arrows indicate hydrocarbon homologs; green arrows indicate expansion of aromatic units

A novel and facile synthesis of 3-(2-benzofuroyl)- and 3,6-bis(2-benzofuroyl)carbazole derivatives

• Wentao Gao,
• Meiru Zheng and
• Yang Li

Beilstein J. Org. Chem. 2011, 7, 1533–1540, doi:10.3762/bjoc.7.180

• investigate structure–activity relationships in various biological tests or photonic applications. The ready availability of starting materials, mild reaction conditions, short reaction times, experimental simplicity and satisfactory yields contribute to the usefulness of this method. The possible biological

Synthesis, reactivity and biological activity of 5-alkoxymethyluracil analogues

• Lucie Brulikova and
• Jan Hlavac

Beilstein J. Org. Chem. 2011, 7, 678–698, doi:10.3762/bjoc.7.80

• ; although some exhibited weak activity. However, all of these results have made a significant and invaluable contribution to the development of new potent antiviral, cytotoxic or antibacterial agents and have elucidated possible structure–activity relationships. Investigated derivatives. Modifications of

Advances in synthetic approach to and antifungal activity of triazoles

• Kumari Shalini,
• Nitin Kumar,
• Sushma Drabu and
• Pramod Kumar Sharma

Beilstein J. Org. Chem. 2011, 7, 668–677, doi:10.3762/bjoc.7.79

• which an azide and an alkyne undergo a 1,3-dipolar cycloaddition reaction in the presence of a catalyst such as copper (Scheme 1) or ruthemium (Scheme 2) [27]. Some new synthetic methods for 1,2,3-triazoles are given below (Scheme 3, Scheme 4) [28][29]. Structure activity relationships have revealed

First synthesis of 2-(benzofuran-2-yl)-6,7-methylene dioxyquinoline-3-carboxylic acid derivatives

• Wentao Gao,
• Jia Liu,
• Yun Jiang and
• Yang Li

Beilstein J. Org. Chem. 2011, 7, 210–217, doi:10.3762/bjoc.7.28

• can be identified in the clinical antitumor agents etoposide, teniposide [21] and lignan lactone podophyllotoxin [22], and structure–activity relationships have shown that the methylenedioxy moiety is fundamental for cytotoxic activity since it can be metabolized by CYP to form metallo–carbene

Synthesis of 3-(quinolin-2-yl)- and 3,6-bis(quinolin-2-yl)-9H-carbazoles

• Yang Li and
• Wentao Gao

Beilstein J. Org. Chem. 2010, 6, 966–972, doi:10.3762/bjoc.6.108

• ) in good yields is reported. These molecules should allow us, in the future, to investigate structure-activity relationships in various biotests. Experimental Melting points (uncorrected) were determined by using a WRS-1B melting point apparatus. The 1H NMR (400 MHz) spectra were recorded on a Bruker

Novel tetracyclic structures from the synthesis of thiolactone-isatin hybrids

• Renate Hazel Hans,
• Hong Su and
• Kelly Chibale

Beilstein J. Org. Chem. 2010, 6, No. 78, doi:10.3762/bjoc.6.78

• this project are the structure-activity relationships delineated from O-4 modified analogues which reportedly display enhanced antimalarial and promising antitubercular activity [15][16]. The other component of the envisaged hybrid, isatin (2) is an intriguing and synthetically versatile scaffold

Synthesis of gem-difluoromethylenated analogues of boronolide

• Jing Lin,
• Xiao-Long Qiu and
• Feng-Ling Qing

Beilstein J. Org. Chem. 2010, 6, No. 37, doi:10.3762/bjoc.6.37

• and an α,β-unsaturated-δ-lactone moiety, making them an attractive target for total syntheses [6][7][8][9][10][11][12][13][14][15][16] since many natural products with a wide range of biological activity contain these structural elements. Noteworthily, structure–activity relationships have

(Pseudo)amide-linked oligosaccharide mimetics: molecular recognition and supramolecular properties

• José L. Jiménez Blanco,
• Fernando Ortega-Caballero,
• Carmen Ortiz Mellet and
• José M. García Fernández

Beilstein J. Org. Chem. 2010, 6, No. 20, doi:10.3762/bjoc.6.20

• modelling techniques. The results have shown that, in many cases, the three-dimensional structure of naturally occurring biomolecules can be mimicked by carbopeptoids and pseudoamide-linked oligomeric surrogates. Nevertheless, further investigations are required to clarify the structure-activity

• relationships in order to design novel biologically active analogues of potential therapeutic value. Schematic representation of sugar aminoacids (SAAs) and (pseudo)amide oligosaccharide mimetics. Natural SAAs structures and natural nucleosidic antibiotics. The general structure of glycoamino acids and their

A facile synthesis and fungicidal activities of 2-(alkylamino)-5,6-dimethylthieno[2,3-d]pyrimidin- 4(3H)-ones

• Yang-Gen Hu,
• Ai-Hua Zheng,
• Xu-Zhi Ruan and
• Ming-Wu Ding

Beilstein J. Org. Chem. 2008, 4, No. 49, doi:10.3762/bjoc.4.49

• many cases compares favorably with other existing methods. The preliminary bioassay of the compounds indicated that the 2-amino-5,6-dimethylthieno[2,3-d]pyrimidin-4(3H)-ones can be used as lead structure for developing novel fungicides. Further bioassay, optimization and structure-activity

• relationships of the title compounds are underway. Experimental Melting points were uncorrected. MS were measured on a Finnigan Trace MS spectrometer. IR were recorded on a PE-983 infrared spectrometer as KBr pellets with absorption in cm−1. 1H NMR spectra were recorded in CDCl3 on a Varian Mercury 400

Synthesis of crispine A analogues via an intramolecular Schmidt reaction

• Ajoy Kapat,
• Ponminor Senthil Kumar and
• Sundarababu Baskaran

Beilstein J. Org. Chem. 2007, 3, No. 49, doi:10.1186/1860-5397-3-49

• the synthesis of a library of anti-cancer analogues. The structure activity relationships (SAR) and anti-cancer activities of our synthetic derivatives will be reported in due course of time. ORTEP diagram of the acid derivative 4. Epoxide initiated electrophilic cyclization of azide. Crispine A and

Flexible synthesis of poison- frog alkaloids of the 5,8-disubstituted indolizidine- class. II: Synthesis of (-)-209B, (-)-231C, (-)-233D, (-)-235B", (-)-221I, and an epimer of 193E and pharmacological effects at neuronal nicotinic acetylcholine receptors

• Soushi Kobayashi,
• Naoki Toyooka,
• Dejun Zhou,
• Hiroshi Tsuneki,
• Tsutomu Wada,
• Toshiyasu Sasaoka,
• Hideki Sakai,
• Hideo Nemoto,
• H. Martin Garraffo,
• Thomas F. Spande and
• John W. Daly

Beilstein J. Org. Chem. 2007, 3, No. 30, doi:10.1186/1860-5397-3-30

• structure-activity relationships of synthetic 5,8-disubstituted indolizidines at nicotinic subtypes could lead to even more subtype-selective ligands as research probes and as potentially useful drugs. Neuronal nicotinic receptors have been implicated in the physiological processes of reward, cognition

Flexible synthetic routes to poison- frog alkaloids of the 5,8-disubstituted indolizidine- class I: synthesis of common lactam chiral building blocks and application to the synthesis of (-)-203A, (-)-205A, and (-)-219F

• Naoki Toyooka,
• Dejun Zhou,
• Hideo Nemoto,
• H. Martin Garraffo,
• Thomas F. Spande and
• John W. Daly

Beilstein J. Org. Chem. 2007, 3, No. 29, doi:10.1186/1860-5397-3-29

• . Our flexible synthetic strategy provides a powerful tool for the synthesis of 5,8-disubstituted indolizidines, permitting detailed investigation of structure activity relationships for blockade of nAChRs by this class of alkaloids. In this contribution, we describe the synthesis of the common lactam

Reaction of benzoxasilocines with aromatic aldehydes: Synthesis of homopterocarpans

• Míriam Álvarez-Corral,
• Cristóbal López-Sánchez,
• Leticia Jiménez-González,
• Antonio Rosales,
• Manuel Muñoz-Dorado and
• Ignacio Rodríguez-García

Beilstein J. Org. Chem. 2007, 3, No. 5, doi:10.1186/1860-5397-3-5

• would allow the study of structure-activity relationships when compared with the trans isomers. Conclusion The condensation of benzoxasilocines with aromatic aldehydes in the presence of boron trifluoride has been studied. Yields are lower than those for the benzoxasilepines, and the