Search results
Search for "cytotoxic agents" in Full Text gives 13 result(s) in Beilstein Journal of Organic Chemistry.
Photocatalyzed elaboration of antibody-based bioconjugates
Beilstein J. Org. Chem. 2025, 21, 616–629, doi:10.3762/bjoc.21.49
- designed in the context of cancer therapy [1], which combines the precision targeting of monoclonal antibodies (mAbs) with the therapeutic effects of cytotoxic drugs [2]. The ADCs are thus designed to deliver potent cytotoxic agents selectively and directly to cancer cells while minimizing damage to
Facile and diastereoselective arylation of the privileged 1,4-dihydroisoquinolin-3(2H)-one scaffold
Beilstein J. Org. Chem. 2022, 18, 1070–1078, doi:10.3762/bjoc.18.109
- cytotoxic agents. Keywords: 1,4-dihydroisoquinol-3-one; heterocyclic diazo compounds; hydroarylation; Regitz diazo transfer; triflic acid; Introduction Besides being derivatives of (or a precursor to) the 1,2,3,4-tetrahydroisoquinoline core which itself bears a special significance from the standpoint of
- anticancer cytotoxic agents. Diverse bioactive compounds based on the privileged 1,4-DHIQ scaffold. Strategy investigated in this work. Preparation of 3(2H)-isoquinolones 11. aObtained as a 10:1 mixture of regioisomers; purified by crystallization. bEmployed in the next step without purification (not
Microwave-assisted multicomponent reactions in heterocyclic chemistry and mechanistic aspects
Beilstein J. Org. Chem. 2021, 17, 819–865, doi:10.3762/bjoc.17.71
- marketed drugs structured around indole implying its pharmacological significance such as oxypertine (27), ateviridine (28) [47] and spirooxindole-based potent cytotoxic agents 29, 30 and 31 [48]. In 2017, Lin and co-workers [49] designed a TFA-catalyzed three-component reaction for the regioselective
- reaction time of 24 h. A scale protocol adapted with same reaction conditions afforded the product with a better yield of 92% supporting the scale-up strategy with microwaves. The protocol provided an easy admittance to 5-aza-7-deazapurine molecules used as antiviral and cytotoxic agents [101]. The
Combining enyne metathesis with long-established organic transformations: a powerful strategy for the sustainable synthesis of bioactive molecules
Beilstein J. Org. Chem. 2020, 16, 738–755, doi:10.3762/bjoc.16.68
- constitute a broad family of natural macrolides that act as powerful cytotoxic agents against various cancer cell lines. Due to the stereochemical intricacy and high cytotoxicity, these compounds have attracted a great deal of attention from synthetic chemists. The application of an intermolecular enyne
Novel unit B cryptophycin analogues as payloads for targeted therapy
Beilstein J. Org. Chem. 2018, 14, 1281–1286, doi:10.3762/bjoc.14.109
- potential for chemotherapy. Since targeted therapy provides new perspectives for treatment of cancer, new potent analogues of cytotoxic agents containing functional groups for conjugation to homing devices are required. We describe the design, synthesis and biological evaluation of three new unit B
- glycol spacer with a terminal azide results in a complete loss of activity. Docking studies of the novel cryptophycin analogues to β-tubulin provided a rationale for the observed cytotoxicities. Keywords: cryptophycin; cytotoxic agents; novel payloads; tubulin inhibitors; tumour targeting; Introduction
- not better than its parent. In recent years the targeted delivery of cytotoxic agents has emerged as a highly promising method to tackle selectivity issues [36][37][38][39][40]. Cryptophycin-52 and many analogues lack an addressable group to conjugate the toxin to a homing device. For this reason, new
An overview of recent advances in duplex DNA recognition by small molecules
Beilstein J. Org. Chem. 2018, 14, 1051–1086, doi:10.3762/bjoc.14.93
On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site
Beilstein J. Org. Chem. 2018, 14, 930–954, doi:10.3762/bjoc.14.80
- , occurring via urine. Therefore, most conventional cytotoxic agents applied in chemotherapy lack optimum pharmacokinetic properties (ADME) and thus are not very effective to treat malignancies. Moreover, despite the intensive research to construct new cytotoxic drugs, survival rates in most cancers remain
- enormous pool of unspecific cytotoxic agents that can efficiently kill cancer cells. What is currently needed is not to invest so intensively in generating more cytotoxic agents but to re-use and re-cycle available ones and tailor them to be transformed into targeted chemotherapeutics. Along these lines
- exploited for developing targeted cytotoxic agents: Dysregulation of translation initiation factors and regulators [14]. Mutations in epigenetic regulatory genes [15]. Overexpression of surface receptors like HER2R [16], folate receptor [17], GnRH receptor [18][19] and amino acid transporters [20
Synthesis and in vitro biochemical evaluation of oxime bond-linked daunorubicin–GnRH-III conjugates developed for targeted drug delivery
Beilstein J. Org. Chem. 2018, 14, 756–771, doi:10.3762/bjoc.14.64
- antiproliferative activity. Furthermore, the absence of the free ε-amino group additionally reduced the endocrine effect [23][24]. Thus, the 8Lys can be utilized as conjugation site for cytotoxic agents like anthracyclines. In the past decade, a variety of different linkage systems has been carried out including
Synthesis, antimicrobial and cytotoxicity evaluation of new cholesterol congeners
Beilstein J. Org. Chem. 2015, 11, 1922–1932, doi:10.3762/bjoc.11.208
- group of target cholesterols were screened in vitro as cytotoxic agents against the human prostate cancer cell line PC3 using the sulforhodamine B colorimetric (SRB) assay and doxorubicin as positive control (IC50 = 8.8 μM) (Figure 3) [48]. As shown in Figure 3, cholesterol–lactoside conjugate 27
The chemistry of isoindole natural products
Beilstein J. Org. Chem. 2013, 9, 2048–2078, doi:10.3762/bjoc.9.243
- trichlorocarbinol ester. A first biological evaluation showed that 204 displays antifungal activity. However, only 90 µg could be isolated and further biological screening was not possible [151]. Several sponge-derived macrolides have proven to be effective cytotoxic agents [152][153] and one could speculate that
Total synthesis and biological evaluation of fluorinated cryptophycins
Beilstein J. Org. Chem. 2012, 8, 2060–2066, doi:10.3762/bjoc.8.231
- and docetaxel, displayed biological activity even exceeding that of the parent nonfluorinated compounds [16]. The interesting biological profile of fluorinated cytotoxic agents prompted us to synthesize partially fluorinated analogues of cryptophycins. The depsipeptidic character of the cryptophycins
Cyclization of ortho-hydroxycinnamates to coumarins under mild conditions: A nucleophilic organocatalysis approach
Beilstein J. Org. Chem. 2012, 8, 1630–1636, doi:10.3762/bjoc.8.186
- anticoagulants, antifungal agents, antioxidants, or as anthelmintic, hypnotic and cytotoxic agents [1][2][3][4]. Due to their fluorescent properties, coumarins are also widely used as agrochemicals, additives in cosmetics and food, optical brighteners, and dispersed fluorescent and tunable laser-dye optical
An intramolecular inverse electron demand Diels–Alder approach to annulated α-carbolines
Beilstein J. Org. Chem. 2012, 8, 829–840, doi:10.3762/bjoc.8.93
- -carboline alkaloids are quite rare, and only a few natural products isolated to date contain this pyrido[2,3-b]indole (α-carboline, 1, Figure 1) core. The most prominent examples are grossularine-1 (2) and grossularine-2 (3), which are marine cytotoxic agents that were isolated from the tunicate Dendrodoa
Other Beilstein-Institut Open Science Activities
