Facile synthesis of 1-alkoxy-1H-benzo- and 7-azabenzotriazoles from peptide coupling agents, mechanistic studies, and synthetic applications

• Mahesh K. Lakshman,
• Manish K. Singh,
• Mukesh Kumar,
• Raghu Ram Chamala,
• Vijayender R. Yedulla,
• Domenick Wagner,
• Evan Leung,
• Lijia Yang,
• Asha Matin and
• Sadia Ahmad

Beilstein J. Org. Chem. 2014, 10, 1919–1932, doi:10.3762/bjoc.10.200

• properties, particularly against the human pathogen Acanthamoeba that can infect a variety of organs such as brain, eyes, skin, and lungs [4]. Triazole and benzotriazole derivatives have been evaluated as antitumor agents, with several showing high activities [5], and a benzotriazole derivative was shown to

Preparation of new alkyne-modified ansamitocins by mutasynthesis

• Kirsten Harmrolfs,
• Lena Mancuso,
• Binia Drung,
• Florenz Sasse and
• Andreas Kirschning

Beilstein J. Org. Chem. 2014, 10, 535–543, doi:10.3762/bjoc.10.49

• ; antitumor agents; click chemistry; mutasynthesis; natural products; Introduction Although natural products and analogues cover a large portion of the drug market particularly in the treatment of cancer as well as bacterial and viral infections their role in pharmaceutical research has decreased over the

Synthesis of five- and six-membered cyclic organic peroxides: Key transformations into peroxide ring-retaining products

• Alexander O. Terent'ev,
• Dmitry A. Borisov,
• Vera A. Vil’ and
• Valery M. Dembitsky

Beilstein J. Org. Chem. 2014, 10, 34–114, doi:10.3762/bjoc.10.6

• , and antitumor agents. Keywords: cyclic peroxides; 1,2-dioxanes; 1,2-dioxenes; 1,2-dioxolanes; ozonides; 1,2,4,5-tetraoxanes; 1,2,4-trioxanes; 1,2,4-trioxolanes; Introduction Approaches to the synthesis of five and six-membered cyclic peroxides, such as 1,2-dioxolanes I, 1,2,4-trioxolanes (ozonides

Synthesis and characterization of novel bioactive 1,2,4-oxadiazole natural product analogs bearing the N-phenylmaleimide and N-phenylsuccinimide moieties

• Catalin V. Maftei,
• Elena Fodor,
• Peter G. Jones,
• M. Heiko Franz,
• Gerhard Kelter,
• Heiner Fiebig and
• Ion Neda

Beilstein J. Org. Chem. 2013, 9, 2202–2215, doi:10.3762/bjoc.9.259

• -oxadiazoles are widely used in synthetic chemistry, e.g., in the search for antitumor agents. Cancer consists of more than one hundred different diseases, all of which are characterized by the uncontrolled growth and spread of abnormal cells. In this context, the identification of drugs acting as apoptosis

Synthesis of meso-substituted dihydro-1,3-oxazinoporphyrins

• Satyasheel Sharma and
• Mahendra Nath

Beilstein J. Org. Chem. 2013, 9, 496–502, doi:10.3762/bjoc.9.53

• cancers [30]. Thorough literature search revealed that heterocycles containing a dihydro-1,3-oxazine ring system exhibit a wide spectrum of pharmacological activities, for example, acting as antimicrobial [31][32][33], anti-HIV [34], antimalarial [35] or antitumor agents [36][37]. By considering the

Synthesis of 5-(ethylsulfonyl)-2-methoxyaniline: An important pharmacological fragment of VEGFR2 and other inhibitors

• Miroslav Murár,
• Gabriela Addová and
• Andrej Boháč

Beilstein J. Org. Chem. 2013, 9, 173–179, doi:10.3762/bjoc.9.20

• and a structural fragment of 131 compounds possessing different biological activity, mostly described as antitumor agents (112 compounds) as well as cardiovascular agents, ion-channel blockers, nervous-system blockers, anti-inflammatory agents, and antidiabetic, antiosteoporotic or hypolipemic species

A Wittig-olefination–Claisen-rearrangement approach to the 3-methylquinoline-4-carbaldehyde synthesis

• Mukund G. Kulkarni,
• Mayur P. Desai,
• Deekshaputra R. Birhade,
• Yunus B. Shaikh,
• Ajit N. Dhatrak and
• Ramesh Gannimani

Beilstein J. Org. Chem. 2012, 8, 1725–1729, doi:10.3762/bjoc.8.197

• sites in the midgorge and peripheral sites of butyrylcholinesterase (BuChE) [7]. These derivatives are also exploited in the synthesis of DNA binders [8], macrolides [9], antitumor agents [10] and for the treatment of viral and parasitic infections [11]. Though there are a number of quite efficient

Unprecedented deoxygenation at C-7 of the ansamitocin core during mutasynthetic biotransformations

• Tobias Knobloch,
• Gerald Dräger,
• Wera Collisi,
• Florenz Sasse and
• Andreas Kirschning

Beilstein J. Org. Chem. 2012, 8, 861–869, doi:10.3762/bjoc.8.96

• . Keywords: ansamitocins; antibiotics; antitumor agents; mutasynthesis; natural products; Introduction Natural products still play an important role as lead structures for the treatment of infectious diseases and cancer. However, natural products have lost some of their attraction for the development of

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